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 LC50, TGI, and GI50 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 μM. 1-(7-Hydroxy-4-methyl-2-oxoquinolin-1(2H)-yl)-3-(4-methoxylphenyl)urea (5j) was found to have antiproliferative activity with GI50 of 35.1 μM against HeLa (cervix cancer cell line) and 60.4 μM 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.
Highlights
Cancer is a genetic disease that is caused by changes to gene that control the way our cell functions
The substituted phenyl semicarbazide used in the final step was synthesized as per the reported method [21]
Earlier we have reported the synthesis of oxadiazole derivatives from pyrimidine-2-amine that showed efficiently binding to the active site of EGFRTK [35]
Summary
Cancer is a genetic disease that is caused by changes to gene that control the way our cell functions. In all types of cancers some of the body’s cells begin to divide without stopping and spread into the surrounding tissues. There are more than 100 types of cancer [1]. A total of 1,658,370 new cancer cases and 589,430 cancer deaths are projected to occur in the United States in 2015 [2]. Despite the availability of improved drugs and targeted cancer therapies, it is expected that the new cases of cancer will jump to 19.3 million worldwide by 2025 [3]. The types of cancer treatment include surgery, chemotherapy, radiation therapy, immunotherapy, targeted therapy, and hormonal therapy. The demand for relatively more effective and safer agents for the treatment of cancer is today’s need
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