- 1,2,4-Oxadiazoles: a new class of anti-prostate cancer agents.
1,2,4-Oxadiazoles: a new class of anti-prostate cancer agents.
Bioorganic & medicinal chemistry letters (2012-02-14)
Gopal L Khatik, Jasmine Kaur, Varun Kumar, Kulbhushan Tikoo, Vipin A Nair
PMID22326399
ABSTRAKT
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.
MATERIAŁY