Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 2, Pages 966-970Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm201404w
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Funding
- Brazilian CAPES [2303/10-8]
- Region Rhone-Alpes
- Ligue Nationale Contre le Cancer
- CNRS
- Universite Lyon 1 [UMR 5086]
- French ANR
- Hungarian NIH [2010-INT-1101-01]
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A series of 13 disubstituted chromones was synthesized. Two types of substituents, on each side of the scaffold, contributed to both the potency of ABCG2 inhibition and the cytotoxicity. The best compound, 5-(4-bromobenzyloxy)-2-(2-(5-methoxyindolyl)ethyl-1-carbonyl)-4H-chromen-4-one (6g), displayed high-affinity inhibition and low cytotoxicity, giving a markedly high therapeutic index. The chromone derivative specifically inhibited ABCG2 versus other multidrug ABC transporters and was not transported. It constitutes a highly promising candidate for in vivo chemosensitization of ABCG2-expressing tumors.
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