Synthesis and in Vitro Multidrug Resistance Modulating Activity of a Series of Dihydrobenzopyrans and Tetrahydroquinolines
1999; American Chemical Society; Volume: 42; Issue: 11 Linguagem: Inglês
10.1021/jm980517+
ISSN1520-4804
AutoresRomana Hiessböck, Christian Wolf, Elisabeth Richter, Manuela Hitzler, Peter Chiba, Martin Kratzel, Gerhard F. Ecker,
Tópico(s)Bioactive Compounds and Antitumor Agents
ResumoA 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.
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