NDLI: Quinoxaline-substituted chalcones as new inhibitors of breast cancer resistance protein ABCG2: polyspecificity at B-ring position

Content Provider	PubMed Central
Author	Winter, Evelyn Gozzi, Gustavo Jabor Domeneghini, Chiaradia-delatorre Louise Daflon-yunes, Nathalia Raphael, Terreux Gauthier, Charlotte Mascarello, Alessandra Leal, Paulo César Cadena, Silvia M. Yunes, Rosendo Augusto Nunes, Ricardo José Beatriz, Creczynski-pasa Tania Pietro, Attilio Di
Copyright Year	2014
Abstract	A series of chalcones substituted by a quinoxaline unit at the B-ring were synthesized and tested as inhibitors of breast cancer resistance protein-mediated mitoxantrone efflux. These compounds appeared more efficient than analogs containing other B-ring substituents such as 2-naphthyl or 3,4-methylenedioxyphenyl while an intermediate inhibitory activity was obtained with a 1-naphthyl group. In all cases, two or three methoxy groups had to be present on the phenyl A-ring to produce a maximal inhibition. Molecular modeling indicated both electrostatic and steric positive contributions. A higher potency was observed when the 2-naphthyl or 3,4-methylenedioxyphenyl group was shifted to the A-ring and methoxy substituents were shifted to the phenyl B-ring, indicating preferences among polyspecificity of inhibition.
Related Links	http://dx.doi.org/10.2147/DDDT.S56625
Ending Page	619
Starting Page	609
File Format	PDF
ISSN	11778881
e-ISSN	11778881
Journal	Drug Design, Development and Therapy
Volume Number	8
Language	English
Publisher	Dove Medical Press
Publisher Date	2014-05-27
Access Restriction	Open
Rights Holder	Dove Medical Press
Subject Keyword	Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Pharmacology Pharmaceutical Science

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