Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 33, Issue 1, Pages 1516-1528Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2018.1510919
Keywords
Benzofuran-aminoquinazo-lines; cytotoxicity; apoptosis; EGFR-TK; molecular docking
Funding
- University of South Africa
- University of Pretoria
- National Research Foundation in SA
- Higher Institution Center of Excellence from Malaysia Ministry of Higher Education [311/CIPPM/44001005]
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A 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 29.3nM and 31.1nM, respectively) against Gefitinib (IC50=33.1nM). Molecular docking of compounds 10 into EGFR-TK active site suggests that they bind to the region of EGFR like Gefitinib does. [GRAPHICS]
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