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Flavonoid Dimers as Bivalent Modulators for P‐Glycoprotein‐Based Multidrug Resistance: Structure–Activity Relationships |
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| Authors: | Kin‐Fai Chan Dr. Yunzhe Zhao Dr. Toby W. S. Chow Clare S. W. Yan Dik Lung Ma Dr. Brendan A. Burkett Dr. Iris L. K. Wong Dr. Larry M. C. Chow Prof. Tak Hang Chan Prof. |
| Affiliation: | 1. Department of Applied Biology and Chemical Technology and Laboratory of the Institute of Molecular Technology for Drug Discovery and Synthesis, The Hong Kong Polytechnic University, Hong Kong SAR;2. State Key Laboratory in Chinese Medicine and Molecular Pharmacology, Shenzhen (China), Fax: (+852)?2364 9932;3. These two authors contributed equally to this work. |
| Abstract: | Bivalent modulators of P‐glycoprotein : A small library of flavonoid homodimers and heterodimers was synthesized, and their in vitro activity in reversing paclitaxel resistance was evaluated along with structure–activity relationships. SAR trends indicate that flavonoid dimers with nonpolar, hydrophobic, less bulky substituents generally show more potent reversing activity. This will help guide future efforts in the search for more potent compounds.  |
| Keywords: | flavonoid dimers multidrug resistance paclitaxel P‐glycoprotein structure– activity relationships |