Design, Synthesis and Biological Activity of (20S,21S)-7-Cyclohexyl-21-fluorocamptothecin Carbamates as Potential Antitumor Agents.

Haijun Ma, Baobao Chen, Yuan Wang, Chuanhao Wang, Jianzhong Yao, Wannian Zhang, Zhenyuan Miao

Chemistry & biodiversity 2020 Jul

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20S,21S)-7-Cyclohexyl-21-fluorocamptothecin was discovered by a fluorine drug design strategy with potent antitumor activity and increased metabolic stability. In continuous efforts to find novel antitumor agents derived from natural product camptothecin, 20-carbamates of the active compound (20S,21S)-7-cyclohexyl-21-fluorocamptothecin have been designed and synthesized. Among them, one compound with the diethylamino group showed greater antiproliferative activity than the other 20-carbamate derivatives. The following biological activity assays indicated that the above compound is a valuable lead compound with excellent Topo I inhibitory activity and solution stability. © 2020 Wiley-VHCA AG, Zurich, Switzerland.

Citation

Haijun Ma, Baobao Chen, Yuan Wang, Chuanhao Wang, Jianzhong Yao, Wannian Zhang, Zhenyuan Miao. Design, Synthesis and Biological Activity of (20S,21S)-7-Cyclohexyl-21-fluorocamptothecin Carbamates as Potential Antitumor Agents. Chemistry & biodiversity. 2020 Jul;17(7):e2000068