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 de...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.展开更多
基金supported by the National Natural Science Foundation of China(Nos.21472126,21402122)Shanghai Municipal Natural Science Foundation(No.12ZR450200)
文摘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.
