Design, Synthesis, and Molecular Docking Studies of Some New Quinoxaline Derivatives as EGFR Targeting Agents.

Unlabelled: The synthesis of some new quinoxaline derivatives (-) and their structure determination using H NMR, C NMR and mass spectral analysis was described herein. The in vitro anti-cancer activity of the these compounds () revealed that the compound1-((1-(4-bromophenyl)-1-1,2,3-triazol-4-yl)methyl)-2-(tetrazolo[1,5-]quinoxalin-4-yl)pyrazolidine-3,5-dione () has shown promising activity, whereas, compounds 1-((1-phenyl-1-1,2,3-triazol-4-yl)methyl)-2-(tetrazolo[1,5-]quinoxalin-4-yl)pyrazolidine-3,5-dione (), 1-(tetrazolo[1,5-]quinoxalin-4-yl)-2-((1-(-tolyl)-1-1,2,3-triazol-4-yl)methyl)pyrazolidine-3,5-dione (), 1-((1-(3,5-dimethoxyphenyl)-1-1,2,3-triazol-4-yl)methyl)-2-(tetrazolo[1,5-]quinoxalin-4-yl)pyrazolidine-3,5-dione () and 1-((1-(4-nitrophenyl)-1-1,2,3-triazol-4-yl)methyl)-2-(tetrazolo[1,5-]quinoxalin-4-yl)pyrazolidine-3,5-dione () exhibited good to moderate activity against four human cancer cell lines such as HeLa, MCF-7, HEK 293T, and A549 as compared to the doxorubicin. Predominantly, the compound displayed excellent activity over HeLa, MCF-7, HEK 293T, and A549 with IC values of 3.

Indole-2-carboxylic acid derived mono and bis 1,4-disubstituted 1,2,3-triazoles: Synthesis, characterization and evaluation of anticancer, antibacterial, and DNA-cleavage activities.

A series of new indole-2-carboxylic acid derived mono and bis 1,4-disubstituted 1,2,3 triazoles (I(1)-I(6) and I(7)-I(12)) were synthesized and screened for their anticancer (in vitro and in vivo), antibacterial, and DNA cleavage activities. All the synthesized compounds were characterized by spectral studies. The in vitro anticancer screening results revealed that compound I(12) has registered potential activity against MCF-7, HeLa and HEK293 as compared with the standard reference drug Cisplatin.