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Literature summary for 2.1.1.45 extracted from

  • Lu, G.Q.; Li, X.Y.; Mohamed O, K.; Wang, D.; Meng, F.H.
    Design, synthesis and biological evaluation of novel uracil derivatives bearing 1, 2, 3-triazole moiety as thymidylate synthase (TS) inhibitors and as potential antitumor drugs (2019), Eur. J. Med. Chem., 171, 282-296 .
    View publication on PubMed
Search for more literature for 2.1.1.45

Inhibitors

Inhibitors Comment Organism Structure
2,4-dioxo-N-(2-(1-(m-tolyl)-1H-1,2,3-triazol-4-yl)phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-sulfonamide
-
 Homo sapiens
N-(2-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
 Homo sapiens
N-(2-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1, 2,3,4-tetrahydropyrimidine-5-sulfonamide
-
 Homo sapiens
N-(2-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide compound exhibits the most potent activity against A-549 cells (IC50 1.18 microM) and prominent enzyme inhibition. It inhibits A-549 cells proliferation by arresting the cell cycle in the G1/S phase. The inhibitor can downregulate the cycle checkpoint proteins cyclin D1 and cyclin E to inhibit the cell cycle progression, and then induce intrinsic apoptosis by activating caspase-3, and reducing the ratio of bcl-2/bax Homo sapiens
N-(3-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
 Homo sapiens
N-(3-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
 Homo sapiens
N-(3-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
 Homo sapiens
N-(4-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
 Homo sapiens
N-(4-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
 Homo sapiens
N-(4-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P04818
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-
Hep-G2 cell
-
 Homo sapiens
-
OVCAR-3 cell
-
 Homo sapiens
-
SGC-7901 cell
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00013
-
 pH 7.4, 30°C Homo sapiens N-(2-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
0.00045
-
 pH 7.4, 30°C Homo sapiens N-(3-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
0.00056
-
 pH 7.4, 30°C Homo sapiens N-(3-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
0.0006
-
 pH 7.4, 30°C Homo sapiens N-(2-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1, 2,3,4-tetrahydropyrimidine-5-sulfonamide
0.00074
-
 pH 7.4, 30°C Homo sapiens N-(4-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
0.00087
-
 pH 7.4, 30°C Homo sapiens N-(2-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
0.00128
-
 pH 7.4, 30°C Homo sapiens N-(3-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
0.00158
-
 pH 7.4, 30°C Homo sapiens N-(4-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
0.00165
-
 pH 7.4, 30°C Homo sapiens N-(4-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
0.00197
-
 pH 7.4, 30°C Homo sapiens 2,4-dioxo-N-(2-(1-(m-tolyl)-1H-1,2,3-triazol-4-yl)phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-sulfonamide