摘要
Based on our previous work,a series of hydrazone moiety-bearing aminopyrimidines were synthesized.The compounds were evaluated for inhibitory activities against EGFRT790M/L858 R and antiproliferative activities against H1975 and A549 NSCLC cell lines harboring different forms of EGFR.Compounds 7f and7 k exhibited potent and selective activity in inhibition of gefitinib-resistant H1975 cancer cells（IC50;0.45,0.2μmol/L） while were much less active on A549 cancer cells（IC50;52.83,〉100μmol/L）.Both compounds could be served as promising lead compounds for further investigation.
Based on our previous work,a series of hydrazone moiety-bearing aminopyrimidines were synthesized.The compounds were evaluated for inhibitory activities against EGFRT790M/L858 R and antiproliferative activities against H1975 and A549 NSCLC cell lines harboring different forms of EGFR.Compounds 7f and7 k exhibited potent and selective activity in inhibition of gefitinib-resistant H1975 cancer cells（IC50;0.45,0.2μmol/L） while were much less active on A549 cancer cells（IC50;52.83,〉100μmol/L）.Both compounds could be served as promising lead compounds for further investigation.
基金
supported by grants from Science Foundation of Shenyang Pharmaceutical University(No.QNJJ2014502)
