Ansari, A.JJoshi, GYadav, U.PMaurya, A.KAgnihotri, V.KKalra, SKumar, RSingh, SSawant, D.M.2019-10-232024-08-132019-10-232024-08-132019Ansari, A.J; Joshi, G; Yadav, U.P et al. (2019). Exploration of Pd-catalysed four-component tandem reaction for one-pot assembly of pyrazolo[1,5-c]quinazolines as potential EGFR inhibitors. Bioorganic Chemistry. Vol. 93,45206810.1016/j.bioorg.2019.103314https://kr.cup.edu.in/handle/32116/2481A series of pyrazolo[1,5-c]quinazolines as EGFR inhibitors was designed and synthesized by highly efficient and novel multicomponent route involving Pd-catalyzed tandem one-pot four-component reaction. The reaction proceeds with good functional group tolerance under a simple condition with excellent regioselectivity and high efficiency. Target compounds were screened against cancer cell lines MDA-MB-231, A549 and H1299. Of these, 9b and 10b exhibited superior anticancer activity (IC50 < 2.5 ?M) to erlotinib and gefitinib. Synthetics were able to inhibit EGFR mediated kinase activity, induced ROS in cancer cells promoting mitochondrial mediated apoptosis via halting cell cycle progression at G1 phase.en-USAnticancerCatalysisDrug discoveryEGFRMolecular modellingPyrazolo[1,5-c]quinazolinesArticlehttps://www.sciencedirect.com/science/article/abs/pii/S0045206819307850?via%3Dihub