1,2,4-Oxadiazoles: a new class of anti-prostate cancer agents.
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.
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, Mohali, Punjab 160 062, India.
Gopal L
GL
Khatik
Jasmine
J
Kaur
Varun
V
Kumar
Kulbhushan
K
Tikoo
Vipin A
VA
Nair
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D008297:Male; D010069:Oxadiazoles / Q000737:chemistry* / Q000494:pharmacology*; D011467:Prostate / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D011944:Receptors, Androgen / Q000378:metabolism
D000970:Antineoplastic Agents; D010069:Oxadiazoles; D011944:Receptors, Androgen