Inhibition of human dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(substituted-phenyl)-s-triazine s. A quantitative structure-activity relationship analysis.
The inhibitory activity of 101 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(substituted-phenyl)-s-triazines against purified dihydrofolate reductase from human lymphoblastoid cell (WIL 2) has been studied. From the obtained Kiapp values, quantitative structure-activity relationships (QSAR) have been derived. The QSAR from human dihydrofolate reductase are compared with QSAR for triazines inhibiting bovine and murine tumor DHFR, as well with QSAR for their inhibitory action on murine tumor cell culture.
D000818:Animals; D002417:Cattle; D002460:Cell Line; D005493:Folic Acid Antagonists; D006801:Humans; D008214:Lymphocytes / Q000201:enzymology; D008433:Mathematics; D051379:Mice; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000494:pharmacology*
D005493:Folic Acid Antagonists; D014227:Triazines