Antitumor activity of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines.
Basic Information
ID: ALA1128567
Journal: J Med Chem
Title: Antitumor activity of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines.
Authors: Houlihan WJ, Munder PG, Handley DA, Cheon SH, Parrino VA.
Abstract: A series of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines previously reported to be platelet activating factor (PAF) receptor antagonists were evaluated for potential antitumor activity. Several compounds, such as the 5-(4'-tert-butylphenyl) (65), 5-[4'-(trimethylsilyl)phenyl] (69), and 5-(4'-cyclohexylphenyl) (71) analogs showed very good cytotoxicity against several tumor cell lines. 5-[4'-(Piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,1- a]isoquinoline (SDZ 62-434, 53) was more effective on a milligram per kilogram basis than the clinical cytostatic agent edelfosine (1) in increasing survivors and decreasing tumor volume in the oral mouse Meth A fibrosarcoma assay. It was selected for further development and is currently in phase I clinical trials in cancer patients.
CiteXplore: 7830265
DOI: 10.1021/jm00002a004
Patent ID: ┄