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新型拓扑异构酶抑制剂:吴茱萸堿衍生物的合成及其对拓扑异构酶的抑制活性。

New topoisomerases inhibitors: synthesis of rutaecarpine derivatives and their inhibitory activity against topoisomerases.

机构信息

College of Pharmacy, Yeungnam University, Gyeongsan, Korea.

出版信息

Arch Pharm Res. 2012 May;35(5):785-9. doi: 10.1007/s12272-012-0504-1. Epub 2012 May 29.

Abstract

A series of rutaecarpine derivatives were prepared by employing previously reported methods and their inhibitory activities against topoisomerase I and II were evaluated. Among them, strongly cytotoxic 10-bromorutaecarpine and 3-chlororutaecarpine showed strong inhibitory activities against topo I and II.

摘要

采用先前报道的方法制备了一系列蝙蝠葛堿衍生物,并评价了它们对拓扑异构酶 I 和 II 的抑制活性。其中,具有强细胞毒性的 10-溴代蝙蝠葛堿和 3-氯代蝙蝠葛堿对拓扑异构酶 I 和 II 表现出强烈的抑制活性。

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