Design, synthesis and structure-activity relationships of novel taxane-based multidrug resistance reversal agents |
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| Authors: | Ojima Iwao Borella Christopher P Wu Xinyuan Bounaud Pierre-Yves Oderda Cecilia Fumero Sturm Matthew Miller Michael L Chakravarty Subrata Chen Jin Huang Qing Pera Paula Brooks Tracy A Baer Maria R Bernacki Ralph J |
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| Institution: | Department of Chemistry, State University of New York at Stony Brook, Stony Brook, New York 11794-3400, USA. iojima@notes.cc.sunysb.edu |
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| Abstract: | A series of novel taxane-based multidrug resistance (MDR) reversal agents (TRAs) has been designed and synthesized. Structure-activity relationship (SAR) study clearly indicates that modification of the C-7 position with hydrophobic arenecarbonylcinnamoyl groups brings about high potency against drug efflux mediated by P-glycoprotein (P-gp). Six TRAs exhibit ability to modulate a wide range of ATP-binding cassette (ABC) transporters, such as P-gp, multidrug resistance-associated protein 1 (MRP1), and breast cancer resistance protein (BCRP), which may serve as novel broad-spectrum modulators of ABC transporters. |
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