Design, Synthesis and Anti-NSCLC Activity of Hybrids of Anilinopyrimidines and Cinnamic Acids / 中国药学杂志

ABSTRACT

OBJECTIVE: To design and synthesize a series of hybrids of anilinopyrimidines and cinnamic acids and to find powerful anti-non-small cell lung cancer(NSCLC) drug. METHODS: Compounds 3a-3k were synthesized by combining anilinopyrimidines scaffolds and cinnamic acid derivatives through amide bonds, then the anti-NSCLS activity of these compounds was studied by MTT. RESULTS: Their structures were confirmed by MS and 1H-NMR. Most of target compounds displayed higher anti-proliferative activity on EGFR-mutant H1975 cells(IC50=0.83-3.31 μmolL-1) than gefitinib(IC50=8.59 μmolL-1). CONCLUSION: Compound 3b has the best inhibitory effect on H1975 cells. Therefore, 3b may be a potential anti-NSCLC agent for further investigation.