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Design, synthesis, and SAR analysis of cytotoxic sinapyl alcohol derivatives

2005; Elsevier BV; Volume: 14; Issue: 6 Linguagem: Inglês

10.1016/j.bmc.2005.10.056

1464-3391

Hong Bin Zou, Shengyi Dong, Chang Xin Zhou, Li Hu, Yi Hang Wu, Hai Bo Li, Jing Gong, Lian Sun, Xiu Mei Wu, Hua Bai, Bo Fan, Xiao Jiang Hao, Joachim Stöckigt, Yu Zhao,

Synthetic Organic Chemistry Methods

Five series totalling 51 of sinapyl alcohol derivatives were designed and synthesized. Their cytotoxicity analyses were performed on six human tumor cell lines such as PC-3, CNE, KB, A549, BEL-7404, and HeLa. Certain sinapyl alcohol derivatives showed significant cytotoxic activities. Compound 14d exhibited especially potent cytotoxicity against the BEL-7404 cell line with an IC50 value of 0.7 μM, which showed more cytotoxic activity than the positive control, cisplatin. The structure–cytotoxicity relationships were discussed and the CoMFA analysis was performed using the cytotoxic data against HeLa cells as a template.