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Research in Pharmaceutical Sciences، جلد ۱۳، شماره ۴، صفحات ۳۶۰-۳۶۷
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چکیده فارسی مقاله
کلیدواژه‌های فارسی مقاله
عنوان انگلیسی Structure based design and anti-breast cancer evaluation of some novel 4-anilinoquinazoline derivatives as potential epidermal growth factor receptor inhibitors
چکیده انگلیسی مقاله 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.
کلیدواژه‌های انگلیسی مقاله 4-Anilinoquinazoline,Cytotoxic activity,Docking,EGFR.
نویسندگان مقاله | Zahra Haghighijoo
1Pharmaceutical Sciences Research Center, Pharmacy School, Shiraz University of Medical Sciences, Shiraz, I.R. Iran.


| Zahra Rezaei
3Shiraz Institute for Cancer Research, School of Medicine, Shiraz University of Medical Sciences, Shiraz, I.R. Iran.


| Mansooreh Jaberipoor
1Pharmaceutical Sciences Research Center, Pharmacy School, Shiraz University of Medical Sciences, Shiraz, I.R. Iran.


| Samaneh Taheri
1Pharmaceutical Sciences Research Center, Pharmacy School, Shiraz University of Medical Sciences, Shiraz, I.R. Iran.


| Meysam Jani
1Pharmaceutical Sciences Research Center, Pharmacy School, Shiraz University of Medical Sciences, Shiraz, I.R. Iran.


| Soghra Khabnadideh


نشانی اینترنتی http://rps.mui.ac.ir/index.php/jrps/article/view/1842
فایل مقاله اشکال در دسترسی به فایل - ./files/site1/rds_journals/115/article-115-689406.pdf
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زبان مقاله منتشر شده en
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نوع مقاله منتشر شده Original Article
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