Syntheses and biological activity of bisdaunorubicins

被引：30
|
作者：
Zhang, GS
Fang, LY
Zhu, LZ
Sun, DX [1 ]
Wang, PG
机构：
[1] Ohio State Univ, Div Pharmaceut, Coll Pharm, Columbus, OH 43210 USA
[2] Ohio State Univ, Dept Chem & Biochem, Columbus, OH 43210 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 02期
基金：
美国国家科学基金会;
关键词：
bisdaunorubicin; click chemistry; structure-activity relationship; anticancer;
D O I：
10.1016/j.bmc.2005.08.014
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
To study the length and flexibility of the linkers between two monomers of bisdaunorubicins for their activity against cancer cells, seven bisdaunorubicins were rationally designed and synthesized through click chemistry. Their cytotoxicity was tested in leukemia cells with MTS assay. The results showed that the compounds with short linkers exhibited higher activity than the compounds with long linkers, while the flexibility of the linker also contributed to their activity. These results indicated that the length and flexibility of the linkers between two monomers in bisdaunorubicins are very critical to maintain their activity against cancer cells. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：426 / 434
页数：9
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