Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity

…, Y Zhou, M Ng, T Lu, K Lee, K Sangthongpitag…

文献索引：Wang, Haishan; Lim, Ze-Yi; Zhou, Yan; Ng, Melvin; Lu, Ting; Lee, Ken; Sangthongpitag, Kanda; Goh, Kee Chuan; Wang, Xukun; Wu, Xiaofeng; Khng, Hwee Hoon; Goh, Siok Kun; Ong, Wai Chung; Bonday, Zahid; Sun, Eric T. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 11 p. 3314 - 3321

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被引用次数: 14

摘要

Thirty-six novel acylurea connected straight chain hydroxamates were designed and synthesized. Structure–activity relationships (SAR) were established for the length of linear chain linker and substitutions on the benzoylurea group. Compounds 5g, 5i, 5n, and 19 showed 10–20-fold enhanced HDAC1 potency compared to SAHA. In general, the cellular potency pIC50 (COLO205) correlates with enzymatic potency pIC50 (HDAC1). Compound ...