Bioorganic & Medicinal Chemistry Letters 2012-03-01

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

Gopal L Khatik, Jasmine Kaur, Varun Kumar, Kulbhushan Tikoo, Vipin A Nair

文献索引：Bioorg. Med. Chem. Lett. 22(5) , 1912-6, (2012)

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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 IC(50) values ranging from 0.5 to 5.1μM. 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.Copyright © 2012 Elsevier Ltd. All rights reserved.

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