【摘 要】
：
Based on our previous work,a series of hydrazone moiety-bearing aminopyrimidines were synthesized.The compounds were evaluated for inhibitory activities against
【机 构】
：
Key Laboratory of Structure-Based Drug Design and Discovery(Shenyang Pharmaceutical University),Mini
【出 处】
：
Chinese Chemical Letters
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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(IC_(50);0.45,0.2μmol/L) while were much less active on A549 cancer cells(IC_(50);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 forhibitory activities against EGFRT790M / L858 R and antiproliferative activities against H1975 and A549 NSCLC cell lines harboring different forms of EGFR. potent and selective activity in inhibition of gefitinib-resistant H1975 cancer cells (IC_ (50); 0.45, 0.2 μmol / L) while were less active on A549 cancer cells (IC_ (50); 52.83,> 100 μmol / compounds could be served as promising lead compounds for further investigation.
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