Molecular modifications of 2-arylidene-1-indanones leading to increased cytotoxic potencies.
A series of 2-arylidene-1-indanones, 1, had been shown previously to display cytotoxic properties towards Molt 4/C8, CEM and L1210 cells. In the present study, two series of analogues of 1 were prepared namely various 2-arylidene-1,3-indandiones, 2, and chalcones, 3. In general, the potencies of compounds 2 and 3 were greater than the analogues bearing the same aryl substituents in series 1. Molecular modeling was undertaken in order to seek explanations for the variation in bioactivities.
Pati
Hari N
HN
College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan S7N 5C9, Canada.
Das
Umashankar
U
De Clercq
Erik
E
Balzarini
Jan
J
Dimmock
Jonathan R
JR
D000818:Animals; D045744:Cell Line, Tumor; D006801:Humans; D007189:Indans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008958:Models, Molecular
D007189:Indans