Ring-hydroxylated analogs of lucanthone as antitumor agents
- 1 March 1982
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 25 (3) , 220-227
- https://doi.org/10.1021/jm00345a006
Abstract
A series of ring-alkoxylated and ring-hydroxylated analogs of lucanthone was prepared and tested for antitumor activity. The most biologically interesting members of this group were two 7-hydroxylucanthone derivatives [one of which was 1-((2-(dimethylamino)ethyl)amino)-7-hydroxy-4-methylthioxanthenone] which gave T/C values in the NCI [mouse leukemia] P-388 antitumor screen of 188 and 265, respectively. The apparent association constants and .DELTA.Tm [change in melting temperature] values for a number of analog-DNA complexes were determined to ascertain whether there was any quantitative correlation with biological activity. Intercalation may be a necessary but far from sufficient condition for antitumor activity.This publication has 2 references indexed in Scilit:
- Hycanthone,1 a New Active Metabolite of Lucanthone2Journal of Medicinal Chemistry, 1967
- A Systematic Investigation of Thioxanthen-9-ones and Analogs as Potential Antitumor Agents1,2Journal of Medicinal Chemistry, 1963