| Literature DB >> 15771464 |
Iwao Ojima1, Christopher P Borella, Xinyuan Wu, Pierre-Yves Bounaud, Cecilia Fumero Oderda, Matthew Sturm, Michael L Miller, Subrata Chakravarty, Jin Chen, Qing Huang, Paula Pera, Tracy A Brooks, Maria R Baer, Ralph J Bernacki.
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.Entities:
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Year: 2005 PMID： 15771464 DOI： 10.1021/jm049483y
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446