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(2E)-2-([3-methoxy-4-[(1H-tetrazol-5-yl)methoxy]phenyl]methylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2E)-2-benzylidene[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2E)-2-[(2-oxo-1,2-dihydroquinolin-3-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2E)-2-[(5-iodofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
moderate to low inhibition
(2E)-2-[(naphthalen-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2E)-2-[[2,4-bis(4-methylpiperidin-1-yl)-5-nitrophenyl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-benzylidene[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-ethylidene[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(2E)-3-phenylprop-2-en-1-ylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(3-phenoxyphenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(4-chlorophenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(4-iodophenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(4-methylphenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(5-bromofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(5-iodofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
highly selective for NPP1 as compared to other human enzymes, i.e. NPP2, NPP3, NTPDases1-3, TNAP, and eN
(2Z)-2-[(5-methylfuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(5-nitrofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(5-phenylfuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(furan-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(pyridin-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(thiophen-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[[3-(benzyloxy)phenyl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[[4-(morpholin-4-yl)phenyl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[[5-(dimethylamino)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[[5-(phenylsulfanyl)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
-
(3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
-
(3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
-
(3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
-
(4-aminophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
-
(4-aminophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
-
(4-aminophenyl) (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)methanone
-
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (4-chlorophenyl)methanone
-
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
-
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
-
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
-
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (p-tolyl)methanone
-
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
-
(4-chlorophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
-
(4-chlorophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
-
(E)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-3-phenylprop-2-en-1-one
-
(R)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-2-(4-isobutylphenyl)propan-1-one
-
1,1'-(2-(2-bromophenyl)ethene-1,1-diyl)bis(1H-indole)
1-(4-aminobenzoyl)-5-methyl-1H-pyrazol-3(2H)-one
-
1-amino-4-[4-[(4-anilino-6-chloro-1,3,5-triazin-2-yl)amino]-3-sulfoanilino]-9,10-dioxo-9,10-dihydroanthracene-2-sulfonic acid
-
1-[(4-methoxyphenyl)methyl]-1H-benzimidazole
-
10-methoxy-6-(5-methoxy-1H-indol-1-yl)indolo[2,1-a]isoquinoline
-
12-methyl-6(3-methyl-1H-indol-1-yl)indolo[1,2-h][1,7]naphthyridine
-
12-methyl-6-(3-methyl-1H-indol-1-yl)indolo[2,1-a]isoquinoline
-
2',3'-cAMP
-
7% inhibition at 2 mM
2',3'-dialdehyde ATP
-
competitive inhibition
2,3-Butanedione
-
inactivation half-life: 21.8 min at 0.1 mM
2,3-dimercapto-1-propanol
2,3-dimethoxy-12-methyl-6-(3-methyl-1H-indol-1-yl)indolo[2,1-a]isoquinoline
-
2-(trifluoromethyl)-3,4,8-tri(4-(trifluoromethyl)phenyl)quinoline
-
2-MeSADP
competitive inhibition
2-MeSATP
competitive inhibition
2-methylthioadenosine 5'-triphosphate
-
competitive inhibition
2-[4-[(4-fluorobenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-fluorobenzene-1-sulfonate
-
2-[4-[(4-methoxybenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-methoxybenzene-1-sulfonate
-
2-[4-[(4-methylbenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-methylbenzene-1-sulfonate
38.5% inhibition
2-[4-[(4-tert-butylbenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-tert-butylbenzene-1-sulfonate
shows cytotoxicity against MCF-7 and HT-29 cell lines and shows less cytotoxicity on against A-549 cell
2-[4-[(cyclohexanesulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl cyclohexanesulfonate
30.0% inhibition
2-[4-[(dimethylsulfamoyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl dimethylsulfamate
43.7% inhibition
2-[4-[(ethanesulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl ethanesulfonate
35.1% inhibition
2-[4-[(methylsulfamoyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl methylsulfamate
36.0% inhibition
3',5'-cAMP
-
4% inhibition at 2 mM
3'-O-(4-benzoyl)benzoyladenosine 5'-triphosphate
-
competitive inhibition
3,3'-[(2-chlorophenyl)methylene]bis(4-hydroxy-3,4-dihydro-2H-1-benzopyran-2-one)
-
3,4,8-tri(4-fluorophenyl)-2-(trifluoromethyl)quinoline
-
3,4,8-tri([1,1'-biphenyl]-4-yl)-2-(trifluoromethyl)quinoline
-
3,4,8-tri-(3-chlorophenyl)-2-(trifluoromethyl)quinoline
-
3,4,8-tri-m-tolyl-2-(trifluoromethyl)quinoline
-
3,4,8-tri-p-tolyl-2-(trifluoromethyl)quinoline
-
3,4,8-tribromo-2-(trifluoromethyl)quinoline
-
3,4,8-triphenyl-2-(trifluoromethyl)quinoline
-
3,4,8-tris(3,5-dimethylphenyl)-2-(trifluoromethyl)quinoline
-
3,4,8-tris(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
-
3,5-dimethyl-4-(naphthalen-2-yloxy)-1H-pyrazole
-
3,8-dibromo-2-(trifluoromethyl)quinolin-4(1H)-one
3,8-dibromo-4-(piperidin-1-yl)-2-(trifluoromethyl)quinoline
-
3,8-dibromo-4-(pyrrolidin-1-yl)-2-(trifluoromethyl)quinoline
-
3,8-dibromo-4-chloro-2-(trifluoromethyl)quinoline
-
3,8-dibromo-4-N-butylamine-2-(trifluoromethyl)quinoline
-
3,9-difluoro-6-(6-fluoro-1H-indol-1-yl)indolo[2,1-a]isoquinoline
-
3-(3-bromo-4-chloro-2-(trifluoromethyl)quinolin-8-yl)benzonitrile
-
3-bromo-4-chloro-2-(trifluoromethyl)-8-(4-(trifluoromethyl)phenyl)quinoline
-
3-bromo-4-chloro-8-(2,5-dimethoxyphenyl)-2-(trifluoromethyl)quinoline
-
3-bromo-4-chloro-8-(3,5-difluorophenyl)-2-(trifluoromethyl)quinoline
-
3-bromo-4-chloro-8-(3,5-dimethylphenyl)-2-(trifluoromethyl)quinoline
-
3-bromo-4-chloro-8-(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
-
3-bromo-4-chloro-8-(o-tolyl)-2-(trifluoromethyl)quinoline
-
3-bromo-4-chloro-8-(thiophen-3-yl)-2-(trifluoromethyl)quinoline
-
3-bromo-4-chloro-8-phenyl-2-(trifluoromethyl)quinoline
-
3-bromo-4-N-butylamine-8-(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
-
3-chloropentane-2,4-dione
-
3-fluoro-12-methyl-6-(3-methyl-1H-indol-1-yl)indolo[2,1-a]isoquinoline
-
3-fluoro-6-(1H-pyrrolo[2,3-b]pyridin-1-yl)pyrido[3',2':4,5]pyrrolo[2,1-a]isoquinoline
-
3-methyl-2-(4-methylbenzoyl)-1,2-dihydropyrazol-5-one
-
4,4'-diisothiocyanatostilbene-2,2' disulfonic acid
-
P2-purinoceptor antagonist, less potent inhibition, IC50: 0.022 mM
4-(3,8-dibromo-2-(trifluoromethyl)quinolin-4-yl)morpholine
-
4-(3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-6-[(quinoline-8-sulfonyl)oxy]-1-benzothiophen-2-yl)phenyl quinoline-8-sulfonate
28.7 inhibition; 42.5% inhibition
4-(3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-6-[[4-(trifluoromethyl)benzene-1-sulfonyl]oxy]-1-benzothiophen-2-yl)phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-(4-chlorobenzamido)phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
-
4-(4-chlorobenzamido)phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-(4-chlorobenzamido)phenyl 4-fluorobenzene-1-sulfonate
46% inhibition at 0.1 mM
4-(4-chlorobenzamido)phenyl 4-methylbenzene-1-sulfonate
-
4-(4-chlorobenzamido)phenyl 4-tert-butylbenzene-1-sulfonate
-
4-(4-chlorobenzamido)phenyl benzenesulfonate
-
4-chloro-2-(trifluoromethyl)-3,8-bis(4-(trifluoromethyl)phenyl)quinoline
-
4-chloro-3,8-bis(3-methylphenyl)-2-(trifluoromethyl)quinoline
-
4-chloro-3,8-bis(4-(trifluoromethoxy)phenyl)-2-(trifluoromethyl)quinoline
-
4-chloro-3,8-bis(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
-
4-chloro-3,8-diphenyl-2-(trifluoromethyl)quinoline
-
4-chloro-8-(2,5-dimethoxyphenyl)-2-(trifluoromethyl)-3-(4-(trifluoromethyl)phenyl)quinoline
-
4-chloro-8-phenyl-2-(trifluoromethyl)-3-(4-(trifluoromethyl)phenyl)quinoline
-
4-N-butylamine-3,8-bis(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
-
4-[(cycloheptanecarbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
29% inhibition at 0.1 mM; 37% inhibition at 0.1 mM
4-[(cycloheptanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-[(cycloheptanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
39.3% inhibition at 0.1 mM
4-[(cycloheptanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
-
4-[(cycloheptanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
-
4-[(cycloheptanecarbonyl)amino]phenyl benzenesulfonate
-
4-[(cyclohexanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-[(cyclohexanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
-
4-[(cyclohexanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
39% inhibition at 0.1 mM+L345; 43% inhibition at 0.1 mM
4-[(cyclohexanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
-
4-[(cyclohexanecarbonyl)amino]phenyl benzenesulfonate
-
4-[(cyclohexanecarbonyl)amino]phenyl ethanesulfonate
-
4-[(cyclohexanecarbonyl)amino]phenyl methanesulfonate
-
4-[(cyclohexanecarbonyl)amino]phenyl propane-1-sulfonate
-
4-[(cyclooctanecarbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
30% inhibition at 0.1 mM; 30% inhibition at 0.1 mM
4-[(cyclooctanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
29% inhibition at 0.1 mM
4-[(cyclooctanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
35% inhibition at 0.1 mM; 43% inhibition at 0.1 mM
4-[(cyclooctanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
40% inhibition at 0.1 mM; 46% inhibition at 0.1 mM
4-[(cyclooctanecarbonyl)amino]phenyl benzenesulfonate
45% inhibition at 0.1 mM; 47% inhibition at 0.1 mM
4-[(cyclopentanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-[(cyclopentanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
-
4-[(cyclopentanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
-
4-[(cyclopentanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
-
4-[(cyclopentanecarbonyl)amino]phenyl benzenesulfonate
-
4-[(naphthalene-2-carbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
-
4-[(naphthalene-2-carbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-[(naphthalene-2-carbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
-
4-[(naphthalene-2-carbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
49% inhibition at 0.1 mM
4-[(naphthalene-2-carbonyl)amino]phenyl benzenesulfonate
23% inhibition at 0.1 mM; 24% inhibition at 0.1 mM
4-[(quinoline-8-carbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
37% inhibition at 0.1 mM; 42% inhibition at 0.1 mM
5'-O-(boranyl[[hydroxy(phosphonomethyl)phosphoryl]oxy]phosphoryl)adenosine
-
5'-O-[([[dibromo(phosphono)methyl](hydroxy)phosphoryl]oxy)(hydroxy)phosphoryl]-N,N-diethyladenosine
-
5'-phosphoadenosine 3'-phosphate
-
P2-purinoceptor antagonist, less potent inhibitor, IC50: 0.036 mM
5,5'-(propane-1,3-diyl)di(1,3,4-oxadiazole-2(3H)-thione)
-
5-(1H-pyrazol-1-yl)pyrazolo[5,1-a]isoquinoline
-
5-(1H-pyrrol-1-yl)pyrrolo[2,1-a]isoquinoline
-
6-(1H-benzo[d]imidazol-1-yl)benzo[4,5]imidazo[2,1-a]isoquinoline
-
6-(1H-indol-1-yl)indolo[2,1-a]isoquinoline
-
6-(1H-pyrrolo[2,3-b]pyridin-1-yl)pyrido[3',2':4,5]pyrrolo[2,1-a]isoquinoline
-
6-(4-oxo-4,5,6,7-tetrahydro-1H-indol-1-yl)-9,10-dihydroindolo[2,1-a]isoquinolin-11(8H)-one
-
6-(5-cyano-1H-indol-1-yl)-2,3-dimethoxyindolo[2,1,-a]isoquinoline-10-carbonitrile
-
6-(5-cyano-1H-indol-1-yl)-3-fluoroindolo[2,1-a]isoquinoline-10-carbonitrile
-
6-(5-cyano-1H-indol-1-yl)indolo[2,1-a]isoquinoline-10-carbonitrile
-
8,8'-[carbonylbis[azanediyl-3,1-phenylenecarbonylazanediyl(4-methyl-3,1-phenylene)carbonylazanediyl]]di(naphthalene-1,3,5-trisulfonic acid)
-
8,9-dimethoxy-5-(1H-pyrrol-1-yl)pyrrolo[2,1-a]isoquinoline
-
8-(4-methoxyphenyl)-3,4-di-p-tolyl-2-(trifluoromethyl)quinoline
-
8-phenyl-2-(trifluoromethyl)-3,4-bis(4-(trifluoromethyl)phenyl)quinoline
-
8-phenyl-4-(p-tolyl)-2-(trifluoromethyl)-3-(4-(trifluoromethyl)phenyl)quinoline
-
9-fluoro-6-(6-fluoro-1H-indol-1-yl)-2,3-dimethoxyindolo[2,1-a]isoquinoline
-
9-fluoro-6-(6-fluoro-1H-indol-1-yl)-[1,3]dioxolo[4,5-g]indolo[2,1-a]isoquinoline
-
9-fluoro-6-(6-fluoro-1H-indol-1-yl)indolo[2,1-a]isoquinoline
-
acidic fibroblast growth factor
-
potent inhibition at nearly stoichiometric concentrations, Ki: 1.3 nM
-
adenosine
-
competitive inhibition, Ki: 2.7 mM
adenosine 2'-monophosphate
-
8% inhibition at 2 mM
adenosine 3',5'-bisphosphate
-
-
adenosine 3'-monophosphate
adenosine 5'-alpha,beta-methylene-gamma-thiotriphosphate
-
Adenyl-5'-yl imidodiphosphate
adenylic acid
-
competitive inhibition, Ki: 0.036 mM
ADP-ribose
-
47% inhibition at 0.5 mM, competitive type of inhibition
alpha,beta-methylene adenosine 5'-triphosphate
alpha,beta-methylene ADP
-
mixed inhibition
alpha,beta-methylene ATP
-
competitive inhibition
alpha,beta-methyleneadenosine triphosphate
cannot be hydrolyzed and blocks both NTPase and pyrophosphatase activities
alpha-borano-beta,gamma-MetATP
-
AMP(CH)2PP
-
competitive inhibition, Ki: 25 mM
AMP-amidate
-
competitive inhibition, Ki: 30 mM
AMP-PP(S)
-
competitive inhibition, Ki: 33 mM
B4 lectin
-
from Vicia villosa, strong inhibition between 0.002-0.02 mM, specific for hydrolysis of UDP-N-acetyl-alpha-D-galactosamine, reversal by addition of N-acetyl-alpha-D-galactosamine, only weakly inhibitory towards UDP-galactose or UDP-GlcNAc
-
beta,gamma-methyleneadenosine 5'-triphosphate
-
competitive inhibition of formycin 5'-triphosphate hydrolysis, Ki: 0.1 mM
Borate
-
strong inhibition at pH 8.5, not at pH 7.4
CDP-choline
-
62% inhibition at 0.2 mM
coenzyme A
-
90% inhibition at 0.2 mM
CTP
-
potent inhibition at 0.1 mM
cytidine 5'-diphosphate
-
competitive inhibition, Ki: 0.0085 mM
dAMP
-
16% inhibition at 17 mM
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-gamma,delta-methylene-tetraphosphate
-
diadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
-
dialADP
noncompetitive inhibition
diethyldiphosphate
-
inactivation follows apparent first-order kinetics, completely restored by hydroxylamine
EGTA
-
strong inhibition at 1 mM, partially reversed by Mg2+, complete reactivation at 10 mM Ca2+
F-
-
0.01 mM, 54% inhibition
FeSO4
-
42% inhibition at 1 mM in the presence of 0.1 mM o-phenanthroline
gamma-S-adenosine 5'-(alpha,beta-methylene)triphosphate
competitive inhibition
GDP
-
competitive inhibition, Ki: 0.0025 mM
GDP-mannose
-
competitive inhibition of phosphodiesterase activity
GSH
-
40% inhibition at 1 mM
GSSG
-
25% inhibition at 1 mM
guanidine hydrochloride
-
85% inhibition at 4.2 M, complete recovery of activity after dialysis
ITP
-
potent inhibition at 0.1 mM
L-ascorbic acid
-
8% inhibition at 16 mM
L-phenylalanine
-
5 mM, 10% loss of activity
lectin
-
from Wistaria floribunda, inhibition for hydrolysis of UDP-N-acetyl-alpha-D-galactosamine, reversal by addition of N-acetyl-alpha-D-galactosamine
-
N-(3,4-dimethoxyphenyl)-2-[(5-methoxy-3H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]acetamide
-
N-ethyl-5-phenylisoxazolium-3'-sulfonate
-
Woodward's reagent, inactivation half-life: 16 min at 0.05 mM
N-omega-nitro-L-arginine methyl ester
-
enzyme activity is decreased in serum and platelets from N-omega-nitro-L-arginine methyl ester -treated rats
N-[2-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl] sulfuric diamide
i.e. SAR 03004
N-[2-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
N1-butylnicotinamide chloride
-
competitive inhibition, Ki: 0.408 mM
N1-heptylnicotinamide chloride
-
competitive inhibition, Ki: 0.48 mM
N1-hexylnicotinamide chloride
-
competitive inhibition, Ki: 0.629 mM
N1-octylnicotinamide chloride
-
competitive inhibition, Ki: 0.287 mM
N1-pentylnicotinamide chloride
-
competitive inhibition, Ki: 0.297 mM
nicotinamide
-
19% inhibition at 100 mM
NMN
-
10% inhibition at 40 mM
nucleoside monophosphates
-
-
p-hydroxymercuribenzoate
-
60% inhibition at 1 mM, reversal by GSH
p-nitrophenyl 3'-thymidylate
-
15% inhibition at 0.2 mM
p-nitrophenyl 5'-thymidylate
-
15% inhibition at 0.2 mM
P1,P4-bis(5'-adenosyl)-alpha,beta-gamma,delta-bismethylene-tetraphosphate
-
polyoxymetalate PSB-POM141
-
-
pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid
pyridoxal phosphate-6-azophenyl-2',4'disulfonic acid
PZB08513136A
the most potent thioacetamide derivative
SDS
-
partial inactivation at 0.1%, w/v, complete inactivation at 1%, w/v
Sodium fluoride
-
about 30% residual activity at 40 mM sodium fluoride using ATP as substrate, less than 60% residual activity at 40 mM sodium fluoride using ADP or bis(4-nitrophenyl) phosphate as substrate
thiamine diphosphate
-
17% inhibition at 0.2 mM
thiazolobenzimidazolone
and derivatives
TTP
-
70% inhibition at 1 mM
UDP-galactose
-
competitive inhibition, Ki: 29 mM
uridine 5'-diphosphate
-
competitive inhibition, Ki: 0.0012 mM
UTP
-
potent inhibition at 0.1 mM
[TiW11CoO40]8-
i.e. PSB-POM141
-
1,1'-(2-(2-bromophenyl)ethene-1,1-diyl)bis(1H-indole)
-
1,1'-(2-(2-bromophenyl)ethene-1,1-diyl)bis(1H-indole)
-
2,3-dimercapto-1-propanol
-
nearly complete inactivation at 3 mM
2,3-dimercapto-1-propanol
-
complete inhibition at 5 mM
2-mercaptoethanol
-
80% inhibition at 5 mM
2-mercaptoethanol
-
19% inhibition at 4 mM
2-mercaptoethanol
-
90% inhibition at 16 mM
3,8-dibromo-2-(trifluoromethyl)quinolin-4(1H)-one
-
3,8-dibromo-2-(trifluoromethyl)quinolin-4(1H)-one
-
5'-ADP
-
54% inhibition at 2 mM
5'-ADP
-
competitive inhibition, Ki: 0.0019 mM
5'-ADP
-
complete inhibition at 1 mM
5'-ADP
-
inhibition of monomer
5'-ADP
-
less potent inhibitor
5'-AMP
-
73% inhibition at2 mM
5'-AMP
-
competitive inhibition, Ki: 0.037 mM
5'-AMP
-
biphasic kinetics abolished in the presence of 0.2 mM, Ki: 0.015 mM
5'-AMP
-
sigmoid type of inhibition, phosphate abolishes sigmoidal response
5'-AMP
-
29% inhibition at 12 mM
5'-AMP
-
56% inhibition at 2 mM
5'-AMP
-
effective inhibitor, Ki: 0.5 mM
5'-AMP
-
49% inhibition at 40 mM
5'-AMP
-
complete inhibition at 1 mM for monomer, dimer, tetramer, only dimer inhibits at 0.01 mM to 25%
5'-AMP
-
biphasic inhibition, increasing Km, decreasing Vm
adenosine 3'-monophosphate
-
8% inhibition at 2 mM
adenosine 3'-monophosphate
-
Ki: 1 mM
adenosine 5'-sulfate
-
46% inhibition at 2 mM
adenosine 5'-sulfate
-
Ki: 0.052 mM
Adenyl-5'-yl imidodiphosphate
-
competitive inhibition of formycin 5'-triphosphate hydrolysis, Ki: 0.22 mM
Adenyl-5'-yl imidodiphosphate
-
61-78% inhibition at 1 mM
ADP
-
-
ADP
-
competitive inhibition
alpha,beta-metADP
competitive inhibition
alpha,beta-metADP
mixed inhibition type
alpha,beta-metATP
competitive inhibition
alpha,beta-metATP
competitive inhibition
alpha,beta-methylene adenosine 5'-triphosphate
-
61-78% inhibition at 0.3 mM
alpha,beta-methylene adenosine 5'-triphosphate
-
competitive inhibition, Ki: 25 mM
alpha,beta-methylene adenosine 5'-triphosphate
-
25% inhibition at 2 mM
AMP
-
-
AMP
-
competitive inhibition
ATP
-
competitive inhibition of formycin 5'-triphosphate hydrolysis, Ki: 0.1 mM
ATP
-
potent inhibition at 0.1 mM
ATP
-
competitive inhibition
ATP
-
44% inhibition at 2 mM
ATP
-
inhibition of monomer
ATP
-
non-competitive inhibition
benzoyl-ATP
-
benzoyl-ATP
competitive inhibition
Cibacron blue
-
0.1 mM, substrate Ap4A, strong inhibition, NPP1; 0.1 mM, substrate Ap4A, strong inhibition, NPP2
Cibacron blue
0.1 mM, substrate Ap4A, strong inhibition, NPP1
Cu2+
-
1 mM, more than 95% inhibition
Cu2+
-
inhibition at 5 mM
Cu2+
-
50% inhibition at 1.5 mM
Cu2+
-
45% inhibition at 1 mM
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
-
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
-
dialATP
uncompetitive inhibition
diphosphate
-
complete inhibition above 0.1 mM
diphosphate
-
26% inhibition at 10 mM
diphosphate
-
8% inhibition at 2 mM
diphosphate
-
strong inhibition at pH 8.5, not at pH 7.4
dithiothreitol
-
less than 20% residual activity at 40 mM dithiothreitol using ATP as substrate, less than 10% residual activity at 40 mM dithiothreitol using ADP as substrate, less than 50% residual activity at 40 mM dithiothreitol using bis(4-nitrophenyl) phosphate as substrate
dithiothreitol
-
50% inhibition at 2.3 mM
dithiothreitol
-
92% inhibition at 4 mM, reversal to 92% of initial activity by addition of Zn2+
dithiothreitol
-
complete inactivation at 4 mM
EDTA
-
less than 20% residual activity at 40 mM EDTA using ATP as substrate, less than 10% residual activity at 40 mM EDTA using ADP as substrate, about 40% residual activity at 40 mM EDTA using bis(4-nitrophenyl) phosphate as substrate
EDTA
-
abolishes activity and makes enzyme unstable
EDTA
-
50% inhibition at 0.2 mM
EDTA
-
strong inhibition at 1 mM, partially reversed by Mg2+, complete reactivation at 10 mM Ca2+
EDTA
activity can be restored by addition of 2-5 mM ZnCl2 or CaCl2, but only partially by 2-5 mM MgCl2
EDTA
-
EDTA is not able to remove the bound metal ions in ONPP
EDTA
-
0.1 mM, complete inhibition
EDTA
-
at 0.5 mM, EDTA greatly reduces the catalytic activity
EDTA
-
enhanced inhibition at 0.005 mM in the presence of 5 mM glycine
EDTA
-
complete inhibition at 1 mM
EDTA
-
inactivation after 30 min preincubation at 6 mM
EDTA
-
complete inactivation, partially restored by Mg2+, Ca2+
EDTA
-
50% inhibition at 1 mM
EDTA
-
complete inactivation at 2 mM, no reversal by addition of metals
EDTA
-
complete inhibition at 2 mM, partial reactivation by divalent cations
EDTA
activity is restorable by Zn2+
EDTA
-
complete inhibition, reversal for dimer and tetramer by Zn2+
FAD+
-
50% inhibition at 1-2 mM
FAD+
-
79% inhibition at 0.2 mM
GMP
-
Ki: 0.022 mM
GMP
-
complete inhibition at 1 mM
heparin
-
NPP1
Hg2+
-
inhibition at 5 mM
Hg2+
-
25% inhibition at 1 mM
L-cysteine
-
complete inhibition at 4 mM, reversal to 95% of initial activity by addition of Zn2+
L-cysteine
-
complete inactivation at 4 mM
NAD+
-
82% inhibition at 0.2 mM
NAD+
-
competitive inhibition of phosphodiesterase activity
NAD+
-
84% inhibition at 2 mM
NADH
-
14% inhibition at 2 mM
NADH
-
effective inhibition of DPN splitting
NaF
-
82% inhibition at 10 mM
NaF
-
22% inhibition at 45 mM
Ni2+
-
1 mM, more than 95% inhibition
Ni2+
-
inhibition at 5 mM
Ni2+
-
50% inhibition at 2 mM
o-phenanthroline
-
60-90% inhibition at 0.1 mM, reversal by FeSO4
o-phenanthroline
-
complete inactivation at 2 mM, no reversal by addition of metal ions, m-phenanthroline no effect
o-phenanthroline
-
complete inactivation at 2 mM, partial reactivation by divalent cations
phosphate
-
18% inhibition at 2 mM
pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid
-
0.1 mM, substrate p4A, 42% inhibition, NPP2; 0.1 mM, substrate p4A, about 85% inhibition, NPP1
pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid
0.1 mM, substrate Ap4A, about 85% inhibition, NPP3
pyridoxal phosphate-6-azophenyl-2',4'disulfonic acid
-
P2-purinoceptor antagonist, potent inhibitor, IC50: 0.012 mM
pyridoxal phosphate-6-azophenyl-2',4'disulfonic acid
-
complete inhibition above 0.02 mM
Reactive blue 2
-
-
Reactive blue 2
-
P2-purinoceptor antagonist, potent inhibitor, IC50: 0.012 mM
Sodium diphosphate
-
competitive inhibition, Ki: 0.41 mM
Sodium diphosphate
-
66% inhibition at 25 mM
suramin
-
0.1 mM, substrate Ap4A, about 77% inhibition, NPP2; 0.1 mM, substrate p4A, about 70% inhibition, NPP1
suramin
-
0.25 mM, inhibition
suramin
-
a P2 receptor antagonist and an inhibitor of E-NTPDase and NPP1-2 activities
suramin
-
P2-purinoceptor antagonist, less potent inhibitor, IC50: 0.072 mM
UDP-glucose
-
competitive inhibition of phosphodiesterase activity
UDP-glucose
-
competitive inhibition, Ki: 18 mM
UMP
-
competitive inhibition, Ki: 26 mM
UMP
-
11% inhibition at 56 mM
Urea
-
complete inhibition at 4.5 M for monomer, tetramer inactivated at 6 M
Urea
-
progressive inhibition greater 1 M, 80% inhibition at 6 M, dilution or dialysis results in complete restoration of activity
Zn2+
-
1 mM, more than 95% inhibition
Zn2+
-
inhibition at 5 mM
Zn2+
-
50% inhibition at 20 mM
Zn2+
-
above 1-2 mM of EDTA-concentration optimal in restorage, greater values inhibitory
additional information
-
phenylmethylsulfonyl fluoride does not modify the catalytic activity of NPP
-
additional information
-
diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview
-
additional information
diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview
-
additional information
diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview
-
additional information
structure-activity relationships of thiazolo[3,2-a]benzimidazol-3(2H)-one derivatives as selective nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) inhibitors. Inhibition mechanism, overview
-
additional information
structure-activity relationships of thiazolo[3,2-a]benzimidazol-3(2H)-one derivatives as selective nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) inhibitors. Inhibition mechanism, overview
-
additional information
-
structure-activity relationships of thiazolo[3,2-a]benzimidazol-3(2H)-one derivatives as selective nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) inhibitors. Inhibition mechanism, overview
-
additional information
synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors, structure-activity relationships, molecular docking study and analysis, overview; synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors, structure-activity relationships, molecular docking study and analysis, overview
-
additional information
synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors, structure-activity relationships, molecular docking study and analysis, overview; synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors, structure-activity relationships, molecular docking study and analysis, overview
-
additional information
design and synthesis of arylated 2-trifluoromethylquinolines derivatives by site-selective, chemo-selective amination reactions following regioselective Suzuki-Miyaura coupling reactions. Evaluation of their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs (EC 3.6.1.9) and nucleoside triphosphate diphosphohydrolases (NTPDases, EC 3.6.1.15), docking studies to analyze the active binding site of the molecules, overview. The compounds all show negligible inhibition of NTPDases1-3; design and synthesis of arylated 2-trifluoromethylquinolines derivatives by site-selective, chemo-selective amination reactions following regioselective Suzuki-Miyaura coupling reactions. Evaluation of their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs (EC 3.6.1.9) and nucleoside triphosphate diphosphohydrolases (NTPDases, EC 3.6.1.15), docking studies to analyze the active binding site of the molecules, overview. The compounds all show negligible inhibition of NTPDases1-3
-
additional information
design and synthesis of arylated 2-trifluoromethylquinolines derivatives by site-selective, chemo-selective amination reactions following regioselective Suzuki-Miyaura coupling reactions. Evaluation of their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs (EC 3.6.1.9) and nucleoside triphosphate diphosphohydrolases (NTPDases, EC 3.6.1.15), docking studies to analyze the active binding site of the molecules, overview. The compounds all show negligible inhibition of NTPDases1-3; design and synthesis of arylated 2-trifluoromethylquinolines derivatives by site-selective, chemo-selective amination reactions following regioselective Suzuki-Miyaura coupling reactions. Evaluation of their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs (EC 3.6.1.9) and nucleoside triphosphate diphosphohydrolases (NTPDases, EC 3.6.1.15), docking studies to analyze the active binding site of the molecules, overview. The compounds all show negligible inhibition of NTPDases1-3
-
additional information
synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile, structure activity and structure selectivity relationship of 2-benzoyl-5-methyl-1H-pyrazol-3(2H)-one derivatives, overview. The cytotoxic potential of the synthesized pyrazole derivatives is scrutinized against three different cancer cell lines i.e. breast cancer cells (MCF-7), cervical cancer cells (HeLa), and bone marrow lymphoblast cells (K-562). The assay is performed by using MTT (dimethyl-2-thiazolyl-2,5-diphenyl-2H-tetrazolium bromide)-based cell viability assay; synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile, structure activity and structure selectivity relationship of 2-benzoyl-5-methyl-1H-pyrazol-3(2H)-one derivatives, overview. The cytotoxic potential of the synthesized pyrazole derivatives is scrutinized against three different cancer cell lines i.e. breast cancer cells (MCF-7), cervical cancer cells (HeLa), and bone marrow lymphoblast cells (K-562). The assay is performed by using MTT (dimethyl-2-thiazolyl-2,5-diphenyl-2H-tetrazolium bromide)-based cell viability assay
-
additional information
synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile, structure activity and structure selectivity relationship of 2-benzoyl-5-methyl-1H-pyrazol-3(2H)-one derivatives, overview. The cytotoxic potential of the synthesized pyrazole derivatives is scrutinized against three different cancer cell lines i.e. breast cancer cells (MCF-7), cervical cancer cells (HeLa), and bone marrow lymphoblast cells (K-562). The assay is performed by using MTT (dimethyl-2-thiazolyl-2,5-diphenyl-2H-tetrazolium bromide)-based cell viability assay; synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile, structure activity and structure selectivity relationship of 2-benzoyl-5-methyl-1H-pyrazol-3(2H)-one derivatives, overview. The cytotoxic potential of the synthesized pyrazole derivatives is scrutinized against three different cancer cell lines i.e. breast cancer cells (MCF-7), cervical cancer cells (HeLa), and bone marrow lymphoblast cells (K-562). The assay is performed by using MTT (dimethyl-2-thiazolyl-2,5-diphenyl-2H-tetrazolium bromide)-based cell viability assay
-
additional information
a series of raloxifene sulfonate/sulfamate derivatives are designed, synthesized, and tested for inhibitory effect against nucleotide pyrophosphatase/phosphodiesterase-1 and -3 (NPP1 and NPP3) enzymes. The compounds are subjected to cytotoxic studies on various cancer cell lines, and the most potent derivatives are explored for their potency against these cancer cell lines, e.g. HT-29 cells, as well as F180 fibroblasts, inhibition values in percent per 0.01 mM. Structure-activity relationships, molecular modeling of inhibitor binding, overview. Pi-Pi stacking interactions and metal interactions with zinc inside the active site are noticed and contributed towards the inhibitory activity; a series of raloxifene sulfonate/sulfamate derivatives are designed, synthesized, and tested for inhibitory effect against nucleotide pyrophosphatase/phosphodiesterase-1 and -3 (NPP1 and NPP3) enzymes. The compounds are subjected to cytotoxic studies on various cancer cell lines, and the most potent derivatives are explored for their potency against these cancer cell lines, e.g. HT-29 cells, as well as F180 fibroblasts. Structure-activity relationships, molecular modeling of inhibitor binding, overview. Pi-Pi stacking interactions and metal interactions with zinc inside the active site are noticed and contributed towards the inhibitory activity
-
additional information
a series of raloxifene sulfonate/sulfamate derivatives are designed, synthesized, and tested for inhibitory effect against nucleotide pyrophosphatase/phosphodiesterase-1 and -3 (NPP1 and NPP3) enzymes. The compounds are subjected to cytotoxic studies on various cancer cell lines, and the most potent derivatives are explored for their potency against these cancer cell lines, e.g. HT-29 cells, as well as F180 fibroblasts, inhibition values in percent per 0.01 mM. Structure-activity relationships, molecular modeling of inhibitor binding, overview. Pi-Pi stacking interactions and metal interactions with zinc inside the active site are noticed and contributed towards the inhibitory activity; a series of raloxifene sulfonate/sulfamate derivatives are designed, synthesized, and tested for inhibitory effect against nucleotide pyrophosphatase/phosphodiesterase-1 and -3 (NPP1 and NPP3) enzymes. The compounds are subjected to cytotoxic studies on various cancer cell lines, and the most potent derivatives are explored for their potency against these cancer cell lines, e.g. HT-29 cells, as well as F180 fibroblasts. Structure-activity relationships, molecular modeling of inhibitor binding, overview. Pi-Pi stacking interactions and metal interactions with zinc inside the active site are noticed and contributed towards the inhibitory activity
-
additional information
synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-1, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines; synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-3, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines
-
additional information
synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-1, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines; synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-3, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines
-
additional information
-
synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-1, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines; synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-3, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines
-
additional information
NPP3 is not affected by 0.1 mM suramin
-
additional information
there is a decrease in relative expression of NPP3 in brain through rat aging
-
additional information
there is a decrease in relative expression of NPP3 in brain through rat aging
-
additional information
-
no inhibition by gadolinium chloride, levamisole, heparin, and lysophosphatidic acid in the soluble and microsomal fractions
-
additional information
poor inhibition by imidazole at 2 mM
-