Synthesis and anticancer activity studies on some 2-chloro-l,4-bis-(5-substituted-l,3,4-oxadiazol-2-ylmethyleneoxy)phenylene derivatives

摘要

2-Chloro-l,4-phenylenedioxy-bis-acetyl hydrazine 1 on reacting with aromatic carboxylic acids in the presence of phosphorus oxychloride affords 2-chloro-bis-l,3,4-oxadiazoles 3a-f and 4a-d.Aroyl hydrazine 1 on reacting with carbon disulphide under basic condition gives oxadiazole-2-thione 2.Three out of four tested compounds show anticancer activity in the primary anticancer assay.These compounds have been extensively screened against a panel of sixty cancer cell lines derived from leukemia,lung,colon,CNS,melanoma,ovarian,renal,prostate and breast cancer,respectively.It is interesting to note that compounds 3d and 3f show significant anticancer activity against most of the cell lines with GI50 values <100 muM concentrations.