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Synthesis and in vitro multidrug resistance modulating activity of a series of dihydrobenzopyrans and tetrahydroquinolines.

作者信息

Hiessböck R, Wolf C, Richter E, Hitzler M, Chiba P, Kratzel M, Ecker G

机构信息

Institute of Pharmaceutical Chemistry, University of Vienna, Althanstrasse 14, A-1090 Wien, Austria.

出版信息

J Med Chem. 1999 Jun 3;42(11):1921-6. doi: 10.1021/jm980517+.

DOI:10.1021/jm980517+
PMID:10354400
Abstract

A series of dihydrobenzopyrans and tetrahydroquinolines was synthesized and pharmacologically tested for their ability to inhibit P-glycoprotein mediated daunomycin efflux in multidrug resistant CCRF-CEM vcr1000 cells. Several compounds exhibit activities in the range of the reference compounds verapamil and propafenone. Preliminary structure-activity relationship studies propose the importance of high molar refractivity values of the compounds and the presence of an additional basic nitrogen atom.

摘要

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