期刊
CHINESE JOURNAL OF CHEMISTRY
卷 29, 期 3, 页码 504-510出版社
WILEY-BLACKWELL
DOI: 10.1002/cjoc.201190113
关键词
N-(3-arylpropyl)-9,10-dihydro-9-oxo-acridine-4-carboxamides; MDR reversal agents; pharmacophore; phase drug design software; structure-activity relationships; structure elucidation
资金
- All India Council for Technical Education (AICTE)
A novel class of molecules with structure N-(3-arylpropyl)-9,10-dihydro-9-oxoacridine-4-carboxamides (20-29) were designed by generating a pharmacophore for potent MDR reversal activity using phase drug design software. The designed molecules were synthesized by a novel synthesis route and evaluated for their inhibitory effects on the transport activity of P-glycoprotein (P-gp) by standard Hoechst 33342 assay method. Based on the pIC(50) values of ten title compounds screened, three compounds exhibited better activity as compared to Verapamil used as standard.
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