Quantitative structure-activity relationships in 2,5-bis(1-aziridinyl)-p-benzoquinone derivatives against leukemia L-1210
- 1 May 1979
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 22 (5) , 491-496
- https://doi.org/10.1021/jm00191a006
Abstract
Antileukemic activities of more than 30 2,5-bis(1-aziridinyl)-p-benzoquinones were correlated against well-defined physicochemical constants. These compounds were evaluated against lymphoid leukemia L-1210 in BDF1 mice. The best equations obtained exhibited a linear dependence on the hydrophobic constant (.pi.). Characteristic aspects of the equations are that the larger the relative hydrophilicity of the drugs the stronger the antileukemic activity will be and that the more hydrophilic compounds have a greater chemotherapeutic index. Steric and electronic effects were also determined to be important. Based on the correlations, 3 compounds were designed, synthesized and biologically evaluated.This publication has 1 reference indexed in Scilit:
- Potential central nervous system antitumor agents. Aziridinylbenzoquinones. 2Journal of Medicinal Chemistry, 1976