Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:23

Article

Guerra-Bubb, Jennifer M.¹  Bowers, Albert A.¹  Smith, William B.⁴  Paranal, Ronald⁴  Estiu, Guillermina³  Wiest, Olaf³  Bradner, James E.⁴  Williams, Robert M.^1,2 

[1] Colorado State Univ, Dept Chem, Ft Collins, CO 80523 USA

[2] Univ Colorado, Ctr Canc, Aurora, CO 80045 USA

[3] Univ Notre Dame, Dept Chem & Biochem, Notre Dame, IN 46556 USA

[4] Dana Farber Canc Inst, Dept Med Oncol, Boston, MA 02115 USA

关键词: Largazole;    HDAC;    Oxazole;    Isostere;    Conformation;   

DOI  :  10.1016/j.bmcl.2013.06.012

来源: Elsevier

【 摘 要 】

The synthesis of an isosteric analog of the natural product and HDAC inhibitor largazole is described. The sulfur atom in the thizaole ring of the natural product has been replaced with an oxygen atom, constituting an oxazole ring. The biochemical activity and cytotoxicity of this species is described. (C) 2013 Elsevier Ltd. All rights reserved.

【 授权许可】

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