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

Eur J Med Chem. 2014 Mar 3:74:717-25. doi: 10.1016/j.ejmech.2013.06.014.

Xiao-Qin Wu ¹, Cheng Huang ¹, Ying-Ming Jia ¹, Bao-An Song ², Jun Li ³, Xin-Hua Liu ⁴

Affiliations

1 School of Pharmacy, Anhui Medical University, Hefei 230032, PR China.
2 Key Laboratory of Green Pesticide and Agriculture Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China.
3 School of Pharmacy, Anhui Medical University, Hefei 230032, PR China. Electronic address: lijun@ahmu.edu.cn.
4 School of Pharmacy, Anhui Medical University, Hefei 230032, PR China; State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China. Electronic address: xhliuhx@163.com.

PMID: 24119869 DOI: 10.1016/j.ejmech.2013.06.014

Abstract

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.

Keywords

Anticancer activity; Coumarin; Dihydropyrazole; Thio-ethanone.

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