Synthesis and anticancer activities of novel 3,5-disubstituted-1,2,4-oxadiazoles
- Bioorg Med Chem Lett. 2009 May 15;19(10):2739-41. doi: 10.1016/j.bmcl.2009.03.158.
- 1. Birla Institute of Technology and Science, Pilani, India. [email protected]
A series of 3,5-disubstituted-1,2,4-oxadiazoles were synthesized and evaluated for their in vitro anti-proliferative activities against various Cancer cell lines. Formation of 1,2,4-oxadiazole ring was accomplished by the reaction of amidoxime with carboxylic acids. The in vitro cytotoxic effects of 3,5-disubstituted-1,2,4-oxadiazoles have been demonstrated across a wide array of tumor cell types and a few compounds exhibited specificity towards pancreatic (3f, 3h, 3j, and 3k) and prostate (3n) Cancer cells. Among the prepared 3,5-disubstituted-1,2,4-oxadiazoles, compound 3n is the most selective (>450-fold) and compound 3p is the most cytotoxic (10nM) against prostate Cancer cell lines.