Structure based design and anti-breast cancer evaluation of some novel 4-anilinoquinazoline derivatives as potential epidermal growth factor receptor inhibitors

Autor: Zahra Haghighijoo, Zahra Rezaei, Mansooreh Jaberipoor, Samaneh Taheri, Meysam Jani, Soghra Khabnadideh
Jazyk: angličtina
Rok vydání: 2018
Předmět:
Zdroj: Research in Pharmaceutical Sciences, Vol 13, Iss 4, Pp 360-367 (2018)
Druh dokumentu: article
ISSN: 1735-5362
1735-9414
DOI: 10.4103/1735-5362.235163
Popis: Quinazoline is one of the most widespread scaffolds amongst natural and synthetic bioactive compounds. Recently the quinazoline derivatives and in particular the 4-anilinoquinazolines have attracted much attention for their anticancer properties due to their capability to stabilize the kinase activity of epidermal growth factor receptor (EGFR). A series of fifteen previously designed and synthesized 4-anilinoquinazoline analogs (4-18) were evaluated for cytotoxic activity on two breast cancer cell lines (MCF-7 and MDA-MB-468). Ligand efficiency and binding mode studies were also done and evaluated for their potentially EGFR inhibitory effects in comparison with imatinib and erlotinib as reference drugs. Among the tested 4-anilinoquinazolines, compound 11, which contains diethoxy at phenyl ring and morpholino pendants at positions 5 and 7 of the quinazoline ring, demonstrated the most potent biological activity on both cell lines. Our new quinazoline derivatives with different substituents such as cyclic or linear ethers and flour groups may be a promising cytotoxic lead compounds for further anti-breast cancer research.
Databáze: Directory of Open Access Journals
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