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Design, synthesis and in vitro antitumor evaluation of novel pyrazole-benzimidazole derivatives.
Ren, Bo; Liu, Rong-Chun; Ji, Kegong; Tang, Jiang-Jiang; Gao, Jin-Ming.
Afiliación
  • Ren B; Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling, 712100 Shaanxi, PR China.
  • Liu RC; Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling, 712100 Shaanxi, PR China.
  • Ji K; Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling, 712100 Shaanxi, PR China.
  • Tang JJ; Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling, 712100 Shaanxi, PR China. Electronic address: tangjiang11@nwafu.edu.cn.
  • Gao JM; Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling, 712100 Shaanxi, PR China.
Bioorg Med Chem Lett ; 43: 128097, 2021 07 01.
Article en En | MEDLINE | ID: mdl-33979690
A series of novel pyrazole-benzimidazole derivatives (6-42) have been designed, synthesized and evaluated for their in vitro antiproliferative activity against the HCT116, MCF-7 and Huh-7 cell lines. Among them, compounds 17, 26 and 35 showed significant antiproliferative activity against HCT116 cell lines with the IC50 values of 4.33, 5.15 and 4.84 µM, respectively. Moreover, fluorescent staining studies showed compound 17 could induce cancer cells apoptosis. The flow cytometry assay revealed that compound 17 could induce cell cycle arrest at G0/G1 phase. All in all, these consequences suggest that pyrazole-benzimidazole derivatives could serve as promising compounds for further research to develop novel and highly potent cancer therapy agents.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Pirazoles / Bencimidazoles / Diseño de Fármacos / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2021 Tipo del documento: Article

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Pirazoles / Bencimidazoles / Diseño de Fármacos / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2021 Tipo del documento: Article