7-substituted-4-hydroxyquinoline-3-carboxylic acids as inhibitors of dehydrogenase enzymes and of the respiration of Ehrlich ascites tumor cells: multivariate analysis and quantitative structure-activity relationship for polar substituents.
The inhibitory activities of a set of nine 7-substituted-4-hydroxyquinoline-3-carboxylic acids against three dehydrogenase enzymes and one whole cell system (Ehrlich ascites tumor cells) have been subjected to principal component analysis. The results clearly indicate that activity against the whole cell test system cannot directly be attributed to inhibition of the enzymes evaluated. The enzyme systems are reflected by the first component that can be identified with polar and steric parameters while hydrophobic effects are absent. The second component is entirely due to the inhibition of ascites cell respiration that depends primarily on hydrophobicity.
D000704:Analysis of Variance; D000818:Animals; D002264:Carboxylic Acids / Q000494:pharmacology; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism*; D006912:Hydroxyquinolines / Q000494:pharmacology*; D007770:L-Lactate Dehydrogenase / Q000037:antagonists & inhibitors*; D008291:Malate Dehydrogenase / Q000037:antagonists & inhibitors*; D010101:Oxygen Consumption / Q000187:drug effects*; D012995:Solubility; D013329:Structure-Activity Relationship
D002264:Carboxylic Acids; D006912:Hydroxyquinolines; D007770:L-Lactate Dehydrogenase; D008291:Malate Dehydrogenase