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

Authors
Hiessbock, R Wolf, C Richter, E Hitzler, M Chiba, P Kratzel, M Ecker, G
Citation
R. Hiessbock et al., Synthesis and in vitro multidrug resistance modulating activity of a series of dihydrobenzopyrans and tetrahydroquinolines, J MED CHEM, 42(11), 1999, pp. 1921-1926
Citations number
20
Categorie Soggetti
Chemistry & Analysis
Journal title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
00222623 → ACNP
Volume
42
Issue
11
Year of publication
1999
Pages
1921 - 1926
Database
ISI
SICI code
0022-2623(19990603)42:11<1921:SAIVMR>2.0.ZU;2-4
Abstract
A series of dihydrobenzopyrans and tetrahydroquinolines was synthesized and pharmacologically tested for their ability to inhibit P-glycoprotein media ted daunomycin efflux in multidrug resistant CCRF-CEM vcr1000 cells. Severa l compounds exhibit activities in the range of the reference compounds vera pamil and propafenone. Preliminary structure-activity relationship studies propose the importance of high molar refractivity values of the compounds a nd the presence of an additional basic nitrogen atom.