Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a potent multi-acting HDAC, EGFR, and HER2 …

X Cai, HX Zhai, J Wang, J Forrester, H Qu…

Index: Cai, Xiong; Zhai, Hai-Xiao; Wang, Jing; Forrester, Jeffrey; Qu, Hui; Yin, Ling; Lai, Cheng-Jung; Bao, Rudi; Qian, Changgeng Journal of Medicinal Chemistry, 2010 , vol. 53, # 5 p. 2000 - 2009

Full Text: HTML

Citation Number: 119

Abstract

By incorporating histone deacetylase (HDAC) inhibitory functionality into the pharmacophore of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) inhibitors, we synthesized a novel series of compounds with potent, multiacting HDAC, EGFR, and HER2 inhibition and identified 7-(4-(3- ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide 8 (CUDC- ...