چاپ صفحه |  صفحه نخست سامانه |  چکیده مقاله |  نویسندگان |  دانلود مقاله | دانشگاه علوم پزشکی تبریز |
| A new series of 1,3,5-trisubstituted 2-pyrazolines for the inhibition of cyclooxygenase-2 (COX-2) were synthesized. The designed structures include a COX-2 pharmacophore SO2CH3 at the para-position of the phenyl ring located at C-5 of a pyrazoline scaffold. The synthesized compounds were tested for in vitro COX-1/COX-2 inhibition and cell toxicity against human colorectal adenocarcinoma cell lines HT-29. The lead compound (4- chlorophenyl){5-[4-(methanesulfonyl)phenyl]-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl}methanone (16) showed significant COX-2 inhibition (IC50= 0.05�0.01 μM), and antiproliferative activity (IC50=5.46�4.71 μM). Molecular docking studies showed that new pyrazoline-based compounds interact via multiple hydrophobic and hydrogen-bond interactions with key binding site residues of the COX-2 enzyme. |
| نویسنده | نفر چندم مقاله |
|---|---|
| تیمور واحدپور | اول |
| سالار همتی | سوم |
| مریم حمزه میوه رود | چهارم |
| علی اکبر علیزاده | پنجم |
| سیاوش دستمالچی | هفتم |
| نام فایل | تاریخ درج فایل | اندازه فایل | دانلود |
|---|---|---|---|
| Synthesis and Biological Evaluation of 1,3,5-Trisubstituted 2-.pdf | 1400/09/30 | 1636517 | دانلود |
