چاپ صفحه |  صفحه نخست سامانه |  چکیده مقاله |  نویسندگان |  دانلود مقاله | علوم پزشکی کرمانشاه |
| کد مقاله | 7367 |
| عنوان فارسی مقاله | |
| عنوان لاتین مقاله | Phthalimide analogs as probable 15lipoxygenase-1 inhibitors: synthesis biological evaluation and docking studies |
| نوع مقاله | مقاله اصیل (پژوهشی، Original) |
| بالاترین نمایه نامه بینالمللی | ISI |
| سطح مقاله | |
| IF | 1.638 |
| عنوان نشریه | DARU Journal of Pharmaceutical Sciences |
| نوع نشریه | داخلی ایندکس شده |
| شماره نشریه | 23 |
| دوره | 36 |
| تاریخ انتشار شمسی | 1394/04/10 |
| تاریخ انتشار میلادی | 2015 |
| آدرس لینک مقاله/ همایش در شبکه اینترنت | http://www.darujps.com/content/23/1/36 |
| DOI | 10.1186/s40199-015-0118-5 |
| آدرس علمی (Affiliation) نویسنده متقاضی | Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran |
| Background: Recentstudieshavebeenexplainedtheroleoflipoxygenases (LOX) in the origin of cancer. Among the lipoxygenases, the 5-LOX, 12-LOX and 15-LOX are more important in the cause of neoplastic disorders. In the present investigation, a new series of anticancer agents with 1,3,4-thiadiazole and phthalimide substructures were synthesized and their in vitro cytotoxicity was evaluated by MTT assay. Moreover, enzyme inhibitory potency was also assessed by enzymatic protocol towards 15-LOX-1. Molecular docking was performed to explore in silico binding mode of the target compounds. Results: Tested compounds showed a better cytotoxic activity against HT29 cell line (colorectal cancer) in comparison with other cell lines (PC3: prostate carcinoma; SKNMC: neuroblastoma). Unfortunately, all of the tested derivatives rendered lower inhibitory potency than quercetin towards 15-LOX-1. Four hydrogen bonds were detected in docking studies for compound 4d as the most potent derivative in enzymatic assay. Conclusions: The biological results of reported compounds in this research were not so satisfactory. But, further structural modifications are necessary to improve the bioactivity of these derivatives. |
| نویسنده | نفر چندم مقاله | نویسنده مسئول |
|---|---|---|
| علیرضا علی آبادی | اول | بلي |
| احمد محمدی فرانی | دوم | خير |
| فرحناز احمدی | ششم | خير |
| زینب حسین زاده | سوم | خير |
| نام فایل | تاریخ درج فایل | اندازه فایل | دانلود |
|---|---|---|---|
| P5.pdf | 1394/09/02 | 1556222 | دانلود |
