Design, synthesis and anti-proliferative effects in tumor cells of new combretastatin A-4 analogs  被引量:3

Design, synthesis and anti-proliferative effects in tumor cells of new combretastatin A-4 analogs

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作  者:Lei Zhao Jiu-Jiu Zhou Xin-Ying Huang Li-Ping Cheng Wan Pang Zhen-Peng Kai Fan-Hong Wu 

机构地区:[1]School of Chemical and Environmental Engineering, Shanghai Institute of Technology

出  处:《Chinese Chemical Letters》2015年第8期993-999,共7页中国化学快报(英文版)

基  金:supported by the National Natural Science Foundation of China(Nos.21472126,21402122);Shanghai Municipal Natural Science Foundation(No.12ZR450200)

摘  要:A total of 11 novel combretastatin A-4(CA-4) analogs were designed, synthesized, and evaluated for the anti-proliferative effects in tumor cells. The compounds represent four structural classes:(i)hydrogenated derivatives,(ii) ethoxyl derivatives,(iii) amino derivatives and(iv) pro-drugs. Biological evaluations demonstrate that multiple structural features control the biological potency. Three of the compounds, sit-1, sit-2 and sit-3, have potent anti-proliferative activity against multiple cancer cell lines. Their pro-drugs were synthesized to increase water solubility. Structure–activity relationship study and Surflex-Docking were studied in this paper. These results will be useful for the design of new CA-4 analogs that are structurally related to the SAR study.A total of 11 novel combretastatin A-4(CA-4) analogs were designed, synthesized, and evaluated for the anti-proliferative effects in tumor cells. The compounds represent four structural classes:(i)hydrogenated derivatives,(ii) ethoxyl derivatives,(iii) amino derivatives and(iv) pro-drugs. Biological evaluations demonstrate that multiple structural features control the biological potency. Three of the compounds, sit-1, sit-2 and sit-3, have potent anti-proliferative activity against multiple cancer cell lines. Their pro-drugs were synthesized to increase water solubility. Structure–activity relationship study and Surflex-Docking were studied in this paper. These results will be useful for the design of new CA-4 analogs that are structurally related to the SAR study.

关 键 词:analogs proliferative potent structurally completion afford Fmoc solubility cytotoxicity dissolved 

分 类 号:TQ460.1[化学工程—制药化工]

 

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