Quantitative structure-activity relationship study on amsacrine derivatives.
Various biological activities of amsacrine derivatives were analyzed in relation to various physico-chemical parameters. The in vitro activity parameters like DNA-binding and cell inhibition constants were found to have significant correlations but with varying physico-chemical parameters. DNA-binding constants were found to be the function of van der Waals volume and the cell inhibition constant to be the function of the hydrophobic parameter. But the in vivo antitumor activity parameters like optimal dose administered intraperitoneally in mice injected with P388 leukemia cells and the percentage increase in life span of treated animals over that of control animals were not found to be related with any property of the molecules.
Gupta
S P
SP
Birla Institute of Technology and Science, Pilani, India.
Ray
A
A
Handa
A
A
Prabhakar
Y S
YS
Aggarwal
D
D
D000677:Amsacrine / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D002455:Cell Division / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004247:DNA / Q000378:metabolism; D007941:Leukemia P388 / Q000473:pathology; D051379:Mice; D013329:Structure-Activity Relationship
D000677:Amsacrine; D004247:DNA