Design, Synthesis and Biological Activity of (20S, 21S)‐7‐Cyclohexyl‐21‐fluorocamptothecin Carbamates as Potential Antitumor Agents,Chemistry & Biodiversity

当前位置： X-MOL 学术 › Chem. Biodivers. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Design, Synthesis and Biological Activity of (20S, 21S)‐7‐Cyclohexyl‐21‐fluorocamptothecin Carbamates as Potential Antitumor Agents
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2020-06-08 , DOI: 10.1002/cbdv.202000068
Haijun Ma ₁ , Baobao Chen ₂ , Yuan Wang ₁ , Chuanhao Wang ₂ , Jianzhong Yao ₃ , Wannian Zhang _{1,

3} , Zhenyuan Miao ₃

Affiliation

(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.

中文翻译：

(20S, 21S)-7-Cyclohexyl-21-fluorocamptothecin 氨基甲酸酯作为潜在抗肿瘤剂的设计、合成和生物活性

(20S,21S)-7-Cyclohexyl-21-fluorocamptothecin 是通过氟药物设计策略发现的，具有有效的抗肿瘤活性和增加的代谢稳定性。在不断努力寻找源自天然产物喜树碱的新型抗肿瘤剂的过程中，已经设计并合成了活性化合物 (20S,21S)-7-环己基-21-氟喜树碱的 20-氨基甲酸酯。其中，一种具有二乙氨基的化合物显示出比其他 20-氨基甲酸酯衍生物更强的抗增殖活性。以下生物活性测定表明，上述化合物是一种有价值的先导化合物，具有优异的 Topo I 抑制活性和溶液稳定性。

更新日期：2020-06-08

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11