Mphahlele, Malose J.Mmonwa, Mmakwena M.Aro, Abimbola ObemisolaMcGaw, Lyndy JoyChoong, Yee Siew2018-10-222018-10-222018-07-31Mphahlele, M.J., Mmonwa, M.M., Aro, A. et al. 2018, 'Synthesis, biological evaluation and molecular docking of novel indole-aminoquinazoline hybrids for anticancer properties', International Journal of Molecular Sciences, vol. 19, art. 2232, pp. 1-17.1422-006710.3390/ijms19082232http://hdl.handle.net/2263/66994A series of indole-aminoquinazolines was prepared via amination of the 2-aryl-4-chloroquinazolines with the 7-amino-2-aryl-5-bromoindoles. It was then evaluated for cytotoxicity in vitro against human lung cancer (A549), epithelial colorectal adenocarcinoma (Caco-2), hepatocellular carcinoma (C3A), breast adenocarcinoma (MCF-7), and cervical cancer (HeLa) cells. A combination on the quinazoline and indole moieties of a 2-phenyl and 2-(4-fluorophenyl) rings in compound 4b; 2-(4-fluorophenyl) and 3-chlorophenyl rings in compound 4f; or the two 2-(4-fluorophenyl) rings in compound 4g, resulted in significant and moderate activity against the Caco-2 and C3A cell lines. The indole-aminoquinazoline hybrids compounds 4f and 4g induced apoptosis in Caco-2 and C3A cells, and were also found to exhibit moderate (IC50 = 52.5 nM) and significant (IC50 = 40.7 nM) inhibitory activity towards epidermal growth factor receptor (EGFR) against gefitinib (IC50 = 38.9 nM). Molecular docking suggests that 4a–h could bind to the ATP region of EGFR like erlotinib.en© 2018 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license.Indole-aminoquinazolinesCytotoxicityApoptosisEGFR-TKMolecular dockingEpidermal growth factor receptor (EGFR)PotentAgentsGefitinibCancerMedicinal chemistryQuinazoline derivativesHepatocellular carcinoma cellsTyrosine kinase inhibitorGrowth hormone receptor (GHR)Article