Literature

Abstract

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.

DOI： 10.1016/j.bmcl.2011.03.066

Design and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents

Bioorganic & Medicinal Chemistry Letters 2011.0

Design and synthesis of novel 5-phenyl-N-piperidine ethanone containing 4,5-dihydropyrazole derivatives as potential antitumor agents

European Journal of Medicinal Chemistry 2012.0

Synthesis and molecular docking study of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential antitumor agents

Bioorganic & Medicinal Chemistry Letters 2010.0

Dihydropyrazole derivatives as telomerase inhibitors: Structure-based design, synthesis, SAR and anticancer evaluation in vitro and in vivo

European Journal of Medicinal Chemistry 2016.0

Identification of human telomerase inhibitors having the core of N -acyl-4,5-dihydropyrazole with anticancer effects

Bioorganic & Medicinal Chemistry Letters 2016.0

Novel coumarin-dihydropyrazole thio-ethanone derivatives: Design, synthesis and anticancer activity