Preethi Saligrama Devegowda, K. S. Balaji, D. S. Prasanna
2016
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Medicinal Chemistry
Abstract
Quinazolines are very important class of heterocyclic compounds with antitumor properties. In search of novel anti-tumour agents, a series of 4-anilinoquinazolines were synthesized and characterized using proton and carbon-13 nuclear magnetic resonance, Fourier transform infrared and mass spectroscopic techniques. These compounds were evaluated for their cytotoxic effect on Ehrlish Ascities Carcinoma cells using 3-(4,5-Dimethylthiazol- 2-Yl)-2,5-Diphenyltetrazolium Bromide against Ehrlish ascities carcinoma cell lines. Among the tested compounds, compound N-(3-((6,7-dimethoxyquinazoline-4-yl)amino)phenyl)-4-nitrobenzene sulfonamide compound exhibited more potent activity with an IC50 value of 10.29 ± 1.14 μM against EAC cell line. In vivo studies using compound N-(3-((6,7-dimethoxyquinazoline-4-yl)amino)phenyl)-4-nitrobenzene sulfonamide showed that there was reduction in the body weight, ascites volume and decrease in cell number. Mice treated with compound N-(3- ((6,7-dimethoxyquinazoline-4-yl)amino)phenyl)-4-nitrobenzene sulfonamide showed higher survivability compared with that of control treated mice. The cells treated with compound N-(3-((6,7-dimethoxyquinazoline-4-yl)amino) phenyl)-4-nitrobenzene sulfonamide also exhibited typical morphological changes of apoptotic damages. Further, compound N-(3-((6,7-dimethoxyquinazoline-4-yl)amino)phenyl)-4-nitrobenzene sulfonamide induced tumour cell death by activating proapoptotic protein Bax which activates caspase-3 and activated caspase –3 cleaves poly (ADP- ribose) polymerase causes DNA fragmentation. Thus, our results strongly conclude that our compound 4G acts as a anticancer agent by inducing apoptosis in Ehrlish ascites carcinoma cells.