Synthesis, Characterization, andIn VitroAnticancer Evaluation of Novel 2,5-Disubstituted 1,3,4-Oxadiazole Analogue

摘要

In this series, we have synthesised a new 2,5-disubstituted 1,3,4-oxadiazole in search of potential therapeutics for cancer. The anticancer activities were evaluated on a panel of 60 cell lines by the National Cancer Institute according to its own screening protocol. Out of the 24 compounds, 11 were selected and evaluated via single high dose (10−5 M). In the next phase, two compounds have been selected for five-dose assay. The compounds 3-(5-benzyl-1,3,4-oxadiazol-2-yl)quinolin-2(1H)-one18(NSC-776965) and 3-[5-(2-phenoxymethyl-benzoimidazol-1-ylmethyl)-[1,3,4]oxadiazol-2-yl]-2-p-tolyloxy-quinoline27(NSC-776971) showed mean growth percentage of 66.23 and 46.61, respectively, in one-dose assay and their GI50values ranging between 1.41–15.8 μM and 0.40–14.9 μM, respectively, in 5-dose assay.