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Literature summary for 1.1.1.64 extracted from

  • Djigoue, G.B.; Kenmogne, L.C.; Roy, J.; Poirier, D.
    Synthesis of 3-spiromorpholinone androsterone derivatives as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3 (2013), Bioorg. Med. Chem. Lett., 23, 6360-6362.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3alpha,5alpha)-3-([(2R,5S)-2,5-dimethyl-4-[2-(trifluoromethyl)benzene-1-sulfonyl]piperazin-1-yl]methyl)-3-hydroxyandrostan-17-one 48.8-92.0% inhibition at 0.0001-0.001 mM Rattus norvegicus
(3R,5'R,10S,13S)-4',5'-dibenzyl-10,13-dimethyltetradecahydro-6'H-spiro[cyclopenta[a]phenanthrene-3,2'-[1,4]oxazinane]-6',17(2H)-dione 6.2-19.5% inhibition at 0.0001-0.001 mM Rattus norvegicus
(3R,5'R,10S,13S)-5'-benzyl-10,13-dimethyltetradecahydro-6'H-spiro[cyclopenta[a]phenanthrene-3,2'-[1,4]oxazinane]-6',17(2H)-dione 58.2-90.4% inhibition at 0.0001-0.001 mM Rattus norvegicus
(3R,5'S,10S,13S)-4',5'-dibenzyl-10,13-dimethyltetradecahydro-6'H-spiro[cyclopenta[a]phenanthrene-3,2'-[1,4]oxazinane]-6',17(2H)-dione 25.6-87.3% inhibition at 0.0001-0.001 mM Rattus norvegicus
(3R,5'S,10S,13S)-5'-benzyl-10,13-dimethyltetradecahydro-6'H-spiro[cyclopenta[a]phenanthrene-3,2'-[1,4]oxazinane]-6',17(2H)-dione 18.5-63.2% inhibition at 0.0001-0.001 mM Rattus norvegicus
(3S)-3,4-dibenzyl-1-oxa-4-azaspiro[5.5]undecan-2-one 47.3-92.1% inhibition at 0.0001-0.001 mM Rattus norvegicus
(3S)-3-benzyl-1-oxa-4-azaspiro[5.5]undecan-2-one 24.2-24.3% inhibition at 0.0001-0.001 mM Rattus norvegicus
additional information synthesis of 3-spiromorpholinone androsterone derivatives as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3, overview Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
testosterone + NADP+ Rattus norvegicus
-
androstenedione + NADPH + H+
-
r

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
prostate cancer cell
-
Rattus norvegicus
-
testis
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
testosterone + NADP+
-
Rattus norvegicus androstenedione + NADPH + H+
-
r

Synonyms

Synonyms Comment Organism
17beta-HSD3
-
Rattus norvegicus
17beta-hydroxysteroid dehydrogenase type 3
-
Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Rattus norvegicus
NADPH
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000014
-
pH and temperature not specified in the publication Rattus norvegicus (3alpha,5alpha)-3-([(2R,5S)-2,5-dimethyl-4-[2-(trifluoromethyl)benzene-1-sulfonyl]piperazin-1-yl]methyl)-3-hydroxyandrostan-17-one
0.000022
-
pH and temperature not specified in the publication Rattus norvegicus (3R,5'S,10S,13S)-5'-benzyl-10,13-dimethyltetradecahydro-6'H-spiro[cyclopenta[a]phenanthrene-3,2'-[1,4]oxazinane]-6',17(2H)-dione
0.000048
-
pH and temperature not specified in the publication Rattus norvegicus (3R,5'S,10S,13S)-4',5'-dibenzyl-10,13-dimethyltetradecahydro-6'H-spiro[cyclopenta[a]phenanthrene-3,2'-[1,4]oxazinane]-6',17(2H)-dione