Design and synthesis of a biotinylated probe of COX-2 inhibitor nimesulide analog JCC76

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Zhong, Bo¹  Lama, Rati¹  Smith, Kerri M.¹  Xu, Yan¹  Su, Bin^1,2 

[1] Cleveland State Univ, Dept Chem, Coll Sci & Hlth Profess, Cleveland, OH 44115 USA

[2] Cleveland State Univ, Ctr Gene Regulat Hlth & Dis, Coll Sci & Hlth Profess, Cleveland, OH 44115 USA

关键词: COX-2;    Nimesulide;    JCC76;    Biotin;    Probe;   

DOI  :  10.1016/j.bmcl.2011.07.025

来源: Elsevier

【 摘 要 】

JCC76 is a derivative of cyclooxygenase-2(COX-2) selective inhibitor nimesulide and exhibits potent antibreast cancer activity. It selectively induces apoptosis of Her2 positive breast cancer cells. However, the specific molecular targets of JCC76 still remain unclear, which significantly withdraw the further drug development of JCC76. To identify the molecular targets of JCC76, a six carbon linker and biotin conjugated JCC76 probe was designed and synthesized. The anti-proliferation activity of the probe and its analogs was evaluated. Published by Elsevier Ltd.

【 授权许可】

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