Water-soluble camptothecin derivatives that are intrinsic topoisomerase I poisons |
| |
Authors: | Rahier Nicolas J Eisenhauer Brian M Gao Rong Jones Shannon H Hecht Sidney M |
| |
Institution: | Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA. |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|