Department of Pharmacy, School of Medicine, Xi'an Jiaotong University, Xi'an 710061, PR China.
Bioorg Med Chem. 2012 Jul 15;20(14):4405-12. doi: 10.1016/j.bmc.2012.05.034. Epub 2012 May 29.
A novel series of N-aryl salicylamides with a hydroxamic acid moiety at 5-position were synthesized efficiently. Their activities against EGFR kinase and HDACs were evaluated. All compounds displayed inhibitory activity against EGFR and HDACs. The antiproliferative activities of synthesized compounds were evaluated by MTT method against human cancer cell lines A431, A549 and HL-60. Compound 1o showed the most potent inhibitory activity against A431 and A549. Compounds 1k and 1n exhibited higher potency against HL-60 than gefitinib and SAHA. N-Aryl salicylamides with a hydroxamic acid moiety at 5-position is another new HDAC-EGFR dual inhibitors.
高效合成了一系列 5-位带有羟肟酸部分的 N-芳基水杨酰胺类化合物。对它们的 EGFR 激酶和 HDAC 抑制活性进行了评价。所有化合物均表现出对 EGFR 和 HDAC 的抑制活性。通过 MTT 法评价了合成化合物对人癌细胞系 A431、A549 和 HL-60 的增殖抑制活性。化合物 1o 对 A431 和 A549 的抑制活性最强。化合物 1k 和 1n 对 HL-60 的活性比吉非替尼和 SAHA 更高。5-位带有羟肟酸部分的 N-芳基水杨酰胺是另一种新型的 HDAC-EGFR 双重抑制剂。
