5-[4-tert-butylphenylsulfanyl]-2,4-quinazolinediamine

A synthetic small molecule quinazoline derivative featuring a tert-butyl-substituted phenylthio group at the 5-position and diamino groups at the 2 and 4 positions of the quinazoline core. It is a potent inhibitor of dihydrofolate reductase (DHFR), an enzyme critical for folate metabolism and DNA synthesis. The compound has demonstrated nanomolar inhibitory activity against yeast DHFR (IC50 ~8 nM) and micromolar activity against human DHFR (IC50 ~2000 nM). Its primary mechanism is competitive inhibition of DHFR by binding to its active site. This class of compounds is often explored for potential antitumor or antimicrobial properties due to their ability to disrupt nucleotide biosynthesis[3][1][2].

Other names

5-(4-tert-butylphenyl)sulfanylquinazoline-2,4-diamine5-(4-tert-butylphenylthio)quinazoline-2,4-diamine5-{[4-(2-methyl-2-propanyl)phenyl]sulfanyl}-2,4-chinazolindiamin5-{[4-(2-methyl-2-propanyl)phenyl]sulfanyl}-2,4-quinazolinediamine