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

2013; Elsevier BV; Volume: 74; Linguagem: Inglês

10.1016/j.ejmech.2013.06.014

1768-3254

Xiaoqin Wu, Cheng Zhi Huang, Ying‐Ming Jia, Baoan Song, Jun Li, Xinhua Liu,

Cancer therapeutics and mechanisms

A series novel 1-(3-substituted-5-phenyl-4,5-dihydropyrazol-1-yl)-2-thio-ethanone derivatives as potential telomerase inhibitors were designed and synthesized. The bioassays demonstrated that compounds 4a, 4f, 4j and 7b, 7d occupied high antiproliferative activity against SGC-7901, MGC-803, Bcap-37 and HEPG-2 cell lines. By a modified TRAP assay, some title compounds were tested against telomerase, and compound 4f showed the most potent inhibitory activity with IC50 value at 0.92 ± 0.09 μM. The mechanism of antitumor action indicated that title compounds 4f and 7b could suppress cell proliferation through inducing cell cycle arrest in G0/G1 phase.