Antitumor activity of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines.

doi:10.1021/JM00002A004

Paper

Antitumor activity of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines.

Published Jan 20, 1995 · W. Houlihan, P. G. Munder, D. Handley

Journal of medicinal chemistry

Q1 SJR score

42

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1

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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.

In Vitro Study

Study Snapshot

5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines show promising antitumor activity, with 5-[4'-(Piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,1-a]isoquino

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Antitumor activity of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines.

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