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Synthesis, biological evaluation and molecular docking studies of aminochalcone derivatives as potential anticancer agents by targeting tubulin colchicine binding site.
Wang, Guangcheng; Peng, Zhiyun; Zhang, Jiebing; Qiu, Jie; Xie, Zhenzhen; Gong, Zipeng.
Afiliação
  • Wang G; Guizhou Provincial Key Laboratory of Pharmaceutics, State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550004, China; Guizhou Provincial Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Guizhou Medica
  • Peng Z; Guizhou Provincial Key Laboratory of Pharmaceutics, State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550004, China; Guizhou Provincial Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Guizhou Medica
  • Zhang J; College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, China.
  • Qiu J; College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, China.
  • Xie Z; College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, China.
  • Gong Z; Guizhou Provincial Key Laboratory of Pharmaceutics, State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550004, China; School of Pharmacy, Guizhou Medical University, Guiyang 550004, China. Electronic address: gzp4012607@126.com.
Bioorg Chem ; 78: 332-340, 2018 08.
Article em En | MEDLINE | ID: mdl-29627654
A series of aminochalcone derivatives have been synthesized, characterized by HRMS, 1H NMR and 13C NMR and evaluated for their antiproliferative activity against HepG2 and HCT116 human cancer cell lines. The most of new synthesized compounds displayed moderate to potent antiproliferative activity against test cancer cell lines. Among the derivatives, compound 4 displayed potent inhibitory activity with IC50 values ranged from 0.018 to 5.33 µM against all tested cancer cell lines including drug resistant HCT-8/T. Furthermore, this compound showed low cytotoxicity on normal human cell lines (LO2). The in vitro tubulin polymerization assay showed that compound 4 inhibited tubulin assembly in a concentration-dependent manner with IC50 value of 7.1 µM, when compared to standard colchicine (IC50 = 9.0 µM). Further biological evaluations revealed that compound 4 was able to arrest the cell cycle in G2/M phase. Molecular docking study demonstrated the interaction of compound 4 at the colchicine binding site of tubulin. All the results indicated that compound 4 is a promising inhibitor of tubulin polymerization for the treatment of cancer.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Tubulina (Proteína) / Chalcona / Simulação de Acoplamento Molecular / Antineoplásicos Limite: Animals / Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2018 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Tubulina (Proteína) / Chalcona / Simulação de Acoplamento Molecular / Antineoplásicos Limite: Animals / Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2018 Tipo de documento: Article