Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities

Y Zhang, H Fang, J Feng, Y Jia, X Wang…

Index: Zhang, Yingjie; Fang, Hao; Feng, Jinhong; Jia, Yuping; Wang, Xuejian; Xu, Wenfang Journal of Medicinal Chemistry, 2011 , vol. 54, # 15 p. 5532 - 5539

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Citation Number: 32

Abstract

Histone deacetylase (HDAC) has emerged as an attractive target for the development of antitumor agents during the past decade. Previously tetrahydroisoquinoline-bearing hydroxamic acid analogue, ZYJ-25e (1), was identified and validated as a potent histone deacetylase inhibitor (HDACi) with marked in vitro and in vivo antitumor potency. In the present study, further modification of 1 led to another more potent, orally active HDACi, ...