| Literature DB >> 9767651 |
F Bois1, C Beney, A Boumendjel, A M Mariotte, G Conseil, A Di Pietro.
Abstract
Previous studies have shown that flavonoids are modulators of the transmembrane P-glycoprotein (P-gp) which mediates cell multidrug resistance. Some structural elements have been identified which seem to contribute to these compounds' activity. In the present study, a series of halogenated chalcones was prepared to further explore the structural requirements for the P-gp modulation. Four halogenated chalcones have been synthesized and evaluated as potential modulators of P-gp-mediated multidrug resistance of cancer cells by in vitro assays using a purified recombinant domain of the transporter containing the modulator binding site. Halogenated chalcones exhibited high-affinity binding, the 2',4', 6'-trihydroxy-4-iodochalcone behaving as the most potent compound with a KD value in the nanomolar range.Entities:
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Year: 1998 PMID： 9767651 DOI： 10.1021/jm9810194
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446