Benzofuran-appended 4-aminoquinazoline hybrids as epidermal growth factor receptor tyrosine kinase inhibitors: synthesis, biological evaluation and molecular docking studies.
J Enzyme Inhib Med Chem
; 33(1): 1516-1528, 2018 Dec.
Article
em En
| MEDLINE
| ID: mdl-30274538
ABSTRACT
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 29.3 nM and 31.1 nM, respectively) against Gefitinib (IC50 = 33.1 nM). Molecular docking of compounds 10 into EGFR-TK active site suggests that they bind to the region of EGFR like Gefitinib does. [Formula see text].
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Base de dados:
MEDLINE
Assunto principal:
Quinazolinas
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Benzofuranos
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Inibidores Enzimáticos
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Receptores ErbB
Limite:
Humans
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article