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1,2,4-Oxadiazoles: A new class of anti-prostate cancer agents

  作者 Khatik, GL; Kaur, J; Kumar, V; Tikoo, K; Nair, VA  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-5;  页码  1912-1916  
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[摘要]Sulfide and sulfonyl derivatives of 1,2,4-oxadiazoles were synthesized and screened by MTT assay on the prostate cancer cells, DU-145. Six compounds were identified as potential anti-prostate cancer agents with IC50 values ranging from 0.5 to 5.1 mu M. These compounds exhibited good activity on the androgen independent cells PC-3, while the results were moderate on androgen dependent LNCaP cells, suggesting the possibility of a mechanism of action different from that of the bioisosteric bicalutamide. Also a very low cytotoxicity was observed on non-cancerous cells MCF-10A. (c) 2012 Elsevier Ltd. All rights reserved.

 
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