Water-soluble camptothecin derivatives that are intrinsic topoisomerase I poisons.
Water-soluble camptothecin derivatives that are intrinsic topoisomerase I poisons.
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DOI：
10.1021/ol030119n
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发表时间：
2004-01
期刊：
影响因子：
5.2
通讯作者：
Nicolas J. Rahier;B. M. Eisenhauer;Rong Gao;S. H. Jones;S. Hecht
中科院分区：
文献类型：
--
作者：
Nicolas J. Rahier;B. M. Eisenhauer;Rong Gao;S. H. Jones;S. Hecht
[structure: see text] In an effort to improve the water solubility of camptothecin, four 20-O-phosphate and phosphonate analogues have been prepared. These analogues are freely water soluble, stable at physiological pH, and stabilize the human topoisomerase I-DNA covalent binary complex with the same sequence selectivity as camptothecin itself. All four compounds inhibited the growth of yeast expressing human topoisomerase I in an enzyme-dependent fashion.
