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 M. 1-(7-Hydroxy-4-methyl-2-oxoquinolin-1(2H)-yl)-3-(4-methoxylphenyl)urea (5j) was found to have antiproliferative activity with GI 50 of 35.1 M against HeLa (cervix cancer cell line) and 60.4 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.
A series of new quinoline analogues was prepared in two steps. All the synthesized compounds were characterized by IR, NMR and mass spectral data. The anticancer activity was carried out as per the standard protocol and LC 50 , TGI and GI 50 were calculated. 1-(7-Hydroxy-4-methyl-2-oxoquinolin-1(2H)-yl)-3-(4-methoxylphenyl)urea (5j) showed maximum anticancer activity with GI 50 of 35.1 µM against HeLa (cervix cancer cell line) and 60.4 µM against MDA-MB-435 (breast cancer cell line) respectively. A molecular docking study implying epidermal growth factor receptor tyrosine kinase (EGFR-TK) was carried out to observe the binding mode of new quinoline analogues on the active site of EGFR-TK. The compound 5j showed maximum docking score among the series of compounds. The amino acid residues Met793 showed backbone H-bonding with the hydroxyl group, while Asp855 showed side chain H-bonding with aryl NH group.
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