期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 19, 页码 5607-5612出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.032
关键词
Cytochrome P450 3A4; CYP3A4; Pancratistatin; Anticancer agent; Ketoconazole
资金
- NSERC
- McMaster University
Two total syntheses of fully functionalized seco-analogs of the anticancer compound pancratistatin are reported. Structure-activity relationship (SAR) studies identified potent and selective inhibitors of human cytochrome P450 3A4 (CYP3A4) and revealed several core pharmacophoric elements. These studies identify potential roadblocks and will guide the further development of a viable selective clinical pancratistatin derivative. (C) 2009 Elsevier Ltd. All rights reserved.
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