Synthesis and Antiproliferative Activity of Some Quinoline and Oxadiazole Derivatives

Abstract

In continuance of our search for newer antiproliferative agents we report herein the synthesis and antiproliferative studies of two series ( 5a–j and 10a–c ) of heterocyclic compounds. All the new compounds were characterized by IR, NMR, and mass spectral data. The antiproliferative activity of 10 compounds ( 5a–j ) was carried out on HeLa (cervix cancer cell line) and MDA-MB-435 (melanoma) and LC 50 , TGI, and GI 50 were calculated, while the antiproliferative activity of 3 compounds ( 10a–c ) was carried out against nine different panels of nearly 60 cell lines (NCI-60) according to the National Cancer Institute (NCI US) Protocol at 10 μ M. 1-(7-Hydroxy-4-methyl-2-oxoquinolin-1(2 H )-yl)-3-(4-methoxylphenyl)urea ( 5j ) was found to have antiproliferative activity with GI 50 of 35.1 μ M against HeLa (cervix cancer cell line) and 60.4 μ M against MDA-MB-435 (melanoma), respectively. The compounds 10a , 10b , and 10c showed antiproliferative activity with comparatively higher selectivity towards HOP-92 (Non-Small Cell Lung Cancer) with percent growth inhibitions (GIs) of 34.14, 35.29, and 31.59, respectively.