期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 50, 期 9, 页码 2040-2048出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm0613119
关键词
-
资金
- Intramural NIH HHS Funding Source: Medline
- NCI NIH HHS [ST32 CA09634-12, T32 CA009634, U01 CA089566-05, U01 CA089566-01A1, U01 CA089566-06, U01 CA089566-04, U01 CA089566, U01 CA89566, U01 CA089566-02, U01 CA089566-03] Funding Source: Medline
- PHS HHS [C06-14400] Funding Source: Medline
Indenoisoquinolines with lactam substituents such as ethylamino, propylamino, and butylamino have previously demonstrated potent biological activity, but an optimal length has never been established. In the present study, a series of simplified indenoisoquinoline analogues possessing a linker spacing of 0-12 carbon atoms between the lactam nitrogen and the terminal amino group have been prepared, determining that 2-4-atom lengths are optimal for topoisomerase I inhibition and cytotoxicity. Using these lengths, analogues were prepared with the amino group and portions of the linker replaced by a pyridine ring. A three-carbon spacer within the pyridine series still demonstrated potent topoisomerase I inhibition.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据