Novel 5-Methyl-2,4-Disubstitued-Oxazole Derivatives: Synthesis and Anticancer Activity

A series of novel 5-methyl-2,4-disubstitued-oxazole derivatives were synthesized and evaluated for their antitumor activities. The bioassay tests showed that 7-(5-methyl-2-(4-(R)phenyl)oxazol-4-yl)quinoline (R = trifluoromethyl, 2a; fluoro, 2b; chloro) and 2-(5-methyl-2-(4-(trifluoromethyl or fluoro)phenyl)oxazol-4-yl)pyrazine derivatives (4a and 4b) were highly effective against PC-3 cell with the IC50 values ranging from 1.2 to 2.0 μg/mL. 2-(2-(2,4-dichlorophenyl or 2,4-difluoro phenyl)-5-methyloxazol-4-yl)pyrazine (4e and 4f) were highly effective against A431 cell. The IC50 values of 4e and 4f against A431 cell were 2.0 and 1.6 μg/mL, respectively.