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Bioorg Med Chem Lett
; 21(10): 2916-20, 2011 May 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21486698
RESUMO
A series of novel N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential telomerase inhibitors were synthesized. The bioassay tests show that compound 4a exhibited high activity against human gastric cancer cell SGC-7901, liver cancer Hep-G2 and human prostate PC-3 cell lines with IC(50) values of 21.23±0.99, 29.43±0.32 and 30.89±1.07 µM, respectively. All title compounds were assayed for telomerase inhibition by a modified TRAP assay, the results show that compound 4a can inhibit telomerase with IC(50) value of 4.0±0.32 µM. Docking simulation was performed to position compound 4a into the telomerase (3DU6) active site to determine the probable binding model.