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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
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