| dc.contributor.author | Ansari, A.J | |
| dc.contributor.author | Joshi, G | |
| dc.contributor.author | Yadav, U.P | |
| dc.contributor.author | Maurya, A.K | |
| dc.contributor.author | Agnihotri, V.K | |
| dc.contributor.author | Kalra, S | |
| dc.contributor.author | Kumar, R | |
| dc.contributor.author | Singh, S | |
| dc.contributor.author | Sawant, D.M. | |
| dc.date.accessioned | 2019-10-23T04:42:43Z | |
| dc.date.available | 2019-10-23T04:42:43Z | |
| dc.date.issued | 2019 | |
| dc.identifier.citation | Ansari, 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, | en_US |
| dc.identifier.issn | 452068 | |
| dc.identifier.uri | http://kr.cup.edu.in/handle/32116/2481 | |
| dc.description.abstract | A 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_US |
| dc.language.iso | en_US | en_US |
| dc.publisher | Academic Press Inc. | en_US |
| dc.subject | Anticancer | en_US |
| dc.subject | Catalysis | en_US |
| dc.subject | Drug discovery | en_US |
| dc.subject | EGFR | en_US |
| dc.subject | Molecular modelling | en_US |
| dc.subject | Pyrazolo[1,5-c]quinazolines | en_US |
| dc.title | Exploration of Pd-catalysed four-component tandem reaction for one-pot assembly of pyrazolo[1,5-c]quinazolines as potential EGFR inhibitors | en_US |
| dc.type | Article | en_US |
| dc.identifier.doi | 10.1016/j.bioorg.2019.103314 | |
| dc.identifier.url | https://www.sciencedirect.com/science/article/abs/pii/S0045206819307850?via%3Dihub | |
| dc.title.journal | Bioorganic Chemistry | en_US |
| dc.type.accesstype | Closed Access | en_US |
