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Synthesis and cytotoxic activity of chalcone analogues containing a thieno[2,3-d]pyrimidin-2-yl group as the A-ring or B-ring.
Wang, Fu-Cheng; Peng, Bin; Cao, Sheng-Li; Li, Hong-Yun; Yuan, Xiao-Li; Zhang, Ting-Ting; Shi, Ruifeng; Li, Zhuqing; Liao, Ji; Wang, Hailong; Li, Jing; Xu, Xingzhi.
Afiliación
  • Wang FC; Department of Chemistry and Beijing Key Laboratory of DNA Damage Response, Capital Normal University, Beijing 100048, PR China.
  • Peng B; Guangdong Key Laboratory for Genome Stability & Disease Prevention and Carson International Cancer Center and Marshall Laboratory of Biomedical Engineering, Shenzhen University School of Medicine, Shenzhen, Guangdong, 518060, PR China.
  • Cao SL; Department of Chemistry and Beijing Key Laboratory of DNA Damage Response, Capital Normal University, Beijing 100048, PR China. Electronic address: slcao@cnu.edu.cn.
  • Li HY; Department of Chemistry and Beijing Key Laboratory of DNA Damage Response, Capital Normal University, Beijing 100048, PR China.
  • Yuan XL; Department of Chemistry and Beijing Key Laboratory of DNA Damage Response, Capital Normal University, Beijing 100048, PR China.
  • Zhang TT; Department of Chemistry and Beijing Key Laboratory of DNA Damage Response, Capital Normal University, Beijing 100048, PR China.
  • Shi R; Guangdong Key Laboratory for Genome Stability & Disease Prevention and Carson International Cancer Center and Marshall Laboratory of Biomedical Engineering, Shenzhen University School of Medicine, Shenzhen, Guangdong, 518060, PR China.
  • Li Z; Guangdong Key Laboratory for Genome Stability & Disease Prevention and Carson International Cancer Center and Marshall Laboratory of Biomedical Engineering, Shenzhen University School of Medicine, Shenzhen, Guangdong, 518060, PR China.
  • Liao J; Guangdong Key Laboratory for Genome Stability & Disease Prevention and Carson International Cancer Center and Marshall Laboratory of Biomedical Engineering, Shenzhen University School of Medicine, Shenzhen, Guangdong, 518060, PR China.
  • Wang H; College of Life Science and Beijing Key Laboratory of DNA Damage Response, Capital Normal University, Beijing 100048, PR China.
  • Li J; College of Life Science and Beijing Key Laboratory of DNA Damage Response, Capital Normal University, Beijing 100048, PR China.
  • Xu X; Guangdong Key Laboratory for Genome Stability & Disease Prevention and Carson International Cancer Center and Marshall Laboratory of Biomedical Engineering, Shenzhen University School of Medicine, Shenzhen, Guangdong, 518060, PR China. Electronic address: xingzhi.xu@szu.edu.cn.
Bioorg Chem ; 94: 103346, 2020 01.
Article en En | MEDLINE | ID: mdl-31645277
Many natural or synthetic chalcones have potential anti-tumor activity. Here, we synthesized two series of chalcone analogues containing a thieno[2,3-d]pyrimidin-2-yl group and evaluated for their cytotoxic activity towards cultured human lung cancer A549 and colorectal HCT-116 cells. Among them, compound 8d was the most cytotoxic against HCT-116 cells, with an IC50 value of 2.65 µM. Analyses of the phenotypic changes induced by this compound found a dose-dependent accumulation of HCT-116 cells in sub-G1 phase, indicating that compound 8d might induce apoptosis. Furthermore, we found that 8d triggered mitochondrial membrane potential depolarization, promoted reactive oxygen species formation in HCT-116 cells, and increased the percentage of early and late apoptotic cells. Finally, immunoblotting indicated that 8d increased PARP-1 and caspases 3, 7 and 9 cleavage. These data suggest that compound 8d induces apoptosis via the mitochondrial death pathway.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Chalconas / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2020 Tipo del documento: Article

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Chalconas / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2020 Tipo del documento: Article
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