Mphahlele, Malose J.Maluleka, Marole M.Aro, Abimbola ObemisolaMcGaw, Lyndy JoyChoong, Yee Siew2019-02-082019-02-082018Malose J. Mphahlele, Marole M. Maluleka, Abimbola Aro, Lyndy J. McGaw& Yee Siew Choong (2018) Benzofuran–appended 4-aminoquinazoline hybrids as epidermalgrowth factor receptor tyrosine kinase inhibitors: synthesis, biological evaluation and moleculardocking studies, Journal of Enzyme Inhibition and Medicinal Chemistry, 33:1, 1516-1528, DOI:10.1080/14756366.2018.1510919.1475-6366 (print)1475-6374 (online)10.1080/14756366.2018.1510919http://hdl.handle.net/2263/68432A series of 2-arylbenzo[b]furan–appended 4-aminoquinazoline hybrids were prepared and evaluated for cytotoxicity in vitro against the human lung cancer (A549), colorectal adenocarcinoma (Caco-2), hepatocellular carcinoma (C3A) and cervical cancer (HeLa) cell lines. Compounds 10d and 10j exhibited significant cytotoxicity against the C3A and Caco-2 cell lines and induced apoptosis in these cell lines. Likewise, compounds 10d and 10e exhibited significant inhibitory activity towards epidermal growth factor receptor- tyrosine kinase phosphorylation (IC50 values of 29.3 nM and 31.1 nM, respectively) against Gefitinib (IC50¼33.1 nM). Molecular docking of compounds 10 into EGFR-TK active site suggests that they bind to the region of EGFR like Gefitinib does.en© 2018 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/).Benzofuran-aminoquinazolinesCytotoxicityApoptosisEGFR-TKMolecular dockingArticle