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

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

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

J Med Chem. 1999 Jun 3;42(11):1921-6.

PubMed ID

10354400 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Daunorubicin	P-glycoprotein 1	Protein	Humans	Unknown	Substrate Inhibitor Inducer	Details