Journal of Medicinal Chemistry p. 234 - 240 (1995)
Update date:2022-09-26
Topics:
Houlihan, William J.
Munder, Paul G.
Handley, Dean A.
Cheon, Seung H.
Parrino, Vincent A.
A series of 5-aryl-2,3-dihydroimidazo<2,1-a>isoquinolines 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-<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.
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