128982-24-1Relevant academic research and scientific papers
Antitumor Activity of 5-Aryl-2,3-dihydroimidazoisoquinolines
Houlihan, William J.,Munder, Paul G.,Handley, Dean A.,Cheon, Seung H.,Parrino, Vincent A.
, p. 234 - 240 (1995)
A series of 5-aryl-2,3-dihydroimidazoisoquinolines previously reported to be platelet activating factor (PAF) receptor antagonist were evaluated for potential antitumor activity.Several compounds, such as the 5-(4'-tert-butylphenyl) (65), 5- (69), and 5-(4'-cyclohexylphenyl) (71) analogs showed very good cytotoxicity against several tumor cell lines. 5--2,3-dihydroimidazoisoquinoline (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.
5-HETERO-OR ARYL-SUBSTITUTED-IMIDAZO(2,1-A)ISOQUINOLINES AND THEIR USE AS PAF RECEPTOR ANTAGONISTS
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, (2008/06/13)
The invention discloses certain 5-hetero or aryl-substituted-imidazo[2, 1-a]isoquinolines useful as platelet activating factor (PAF) receptor antagonists, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-mediated bronchoconstriction and extravassation and PAF-mediated, endotoxin-induced lung injury, and for controlling hyperreactive airways induced by PAF or allergin. In addition, the invention discloses the use of a select group of said compounds as anti-tumor agents.
