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Research in Pharmaceutical Sciences، جلد ۱۳، شماره ۱، صفحات ۱-۱۱
عنوان فارسی
چکیده فارسی مقاله
کلیدواژه‌های فارسی مقاله
عنوان انگلیسی Design, synthesis, cytotoxicity evaluation and docking studies of 1,2,4-triazine derivatives bearing different arylidene-hydrazinyl moieties as potential mTOR inhibitors
چکیده انگلیسی مقاله Mammalian target of rapamycin (mTOR) is a phosphoinositide 3-kinase-related protein kinase which controls cell growth and is frequently deregulated in many cancers. Therefore, mTOR inhibitors are used as antineoplastic agents for cancer treatment. In this study, 1,2,4-triazine derivatives containing different arylidene-hydrazinyl moieties were designed and synthesized. Cytotoxicity of the compounds was evaluated on HL-60 and MCF-7 cell lines by MTT assay. S1 , S2 and S3 exhibited good cytotoxic activity on both cell lines with an IC 50 range of 6.42 - 20.20 μM. In general, substitution of a five-membered heterocyclic ring containing NO 2 , such as 5-nitrofuran-2-yl, resulted in the best potency. Molecular docking analysis was performed to study the possible interactions and binding modes of all the triazine derivatives with mTOR receptor. The most promising compound, S1 , was well accommodated within the active site and had the least estimated free energy of binding (even less than the inherent ligand of the protein, PDB ID: 4JT6). It is concluded from both MTT assay and docking studies that the arylidene moiety linked to the hydrazinyl part of the structure had a prominent role in cytotoxicity and mTOR inhibitory activity.
کلیدواژه‌های انگلیسی مقاله Cancer,mTOR inhibitor,1,2,4-Triazines,Docking,MTT
نویسندگان مقاله سارا رنجبر | sara ranjbar
2medicinal and natural products chemistry research center, shiraz university of medical sciences, shiraz, i.r. iran.

سازمان اصلی تایید شده: دانشگاه علوم پزشکی شیراز (Shiraz university of medical sciences)

نجمه ادراکی | najmeh edraki
2medicinal and natural products chemistry research center, shiraz university of medical sciences, shiraz, i.r. iran.

سازمان اصلی تایید شده: دانشگاه علوم پزشکی شیراز (Shiraz university of medical sciences)

مه سیما khoshneviszadeh | mahsima khoshneviszadeh
3department of medicinal chemistry, faculty of pharmacy, tehran university of medical sciences, tehran, i.r. iran.

سازمان اصلی تایید شده: دانشگاه علوم پزشکی تهران (Tehran university of medical sciences)

علیرضا فرومدی | alireza foroumadi
2medicinal and natural products chemistry research center, shiraz university of medical sciences, shiraz, i.r. iran.

سازمان اصلی تایید شده: دانشگاه علوم پزشکی شیراز (Shiraz university of medical sciences)

رامین میری | ramin miri
1department of medicinal chemistry, school of pharmacy, shiraz university of medical sciences, shiraz, i.r. iran. 2medicinal and natural products chemistry research center, shiraz university of medical sciences, shiraz, i.r. iran.

سازمان اصلی تایید شده: دانشگاه علوم پزشکی شیراز (Shiraz university of medical sciences)

مهدی khoshneviszadeh | mehdi khoshneviszadeh


نشانی اینترنتی http://rps.mui.ac.ir/index.php/jrps/article/view/1800
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زبان مقاله منتشر شده en
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نوع مقاله منتشر شده Original Article
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