Exploration of Pd-catalysed four-component tandem reaction for one-pot assembly of pyrazolo[1,5-c]quinazolines as potential EGFR inhibitors.
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ID: 58786
2019
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 (IC < 2.5 μM) 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.
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ansari2019explorationbioorganic
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| Authors | Ansari, Arshad J;Joshi, Gaurav;Yadav, Umesh Prasad;Maurya, Antim K;Agnihotri, Vijai K;Kalra, Sourav;Kumar, Raj;Singh, Sandeep;Sawant, Devesh M; |
| Journal | Bioorganic chemistry |
| Year | 2019 |
| DOI | S0045-2068(19)30785-0 |
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