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Your search keyword '"Teymour Vahedpour"' showing total 2 results
Start Over Author "Teymour Vahedpour" Topic general chemistry
2 results on '"Teymour Vahedpour"'

2. Synthesis and Biological Evaluation of 1,3,5-Trisubstituted 2-Pyrazolines as Novel Cyclooxygenase-2 Inhibitors with Antiproliferative Activity

Author

Siavoush Dastmalchi, Salar Hemmati, Teymour Vahedpour, Jatinder Kaur, Maryam Hamzeh-Mivehroud, Ali Akbar Alizadeh, and Frank Wuest

Subjects
Stereochemistry, Bioengineering, Pyrazoline, Antineoplastic Agents, 01 natural sciences, Biochemistry, chemistry.chemical_compound, Structure-Activity Relationship, Humans, Binding site, Molecular Biology, IC50, Cell Proliferation, chemistry.chemical_classification, biology, Cyclooxygenase 2 Inhibitors, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, General Chemistry, General Medicine, In vitro, 0104 chemical sciences, Molecular Docking Simulation, 010404 medicinal & biomolecular chemistry, Enzyme, chemistry, Cyclooxygenase 2, biology.protein, Molecular Medicine, Pyrazoles, Cyclooxygenase, Pharmacophore, Drug Screening Assays, Antitumor, Lead compound, HT29 Cells
Abstract

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 SO2 CH3 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.

Published
2020

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