Publications by authors named "Shaimaa A Moussa"
Article Synopsis
- - The traditional "one drug, one target, one illness" approach has limitations for Alzheimer's disease (AD), prompting researchers to explore multi-target directed ligands (MTDLs) as new therapeutic options.
- - Researchers synthesized new coumarin derivatives and found that compounds 6c and 6h were particularly effective as inhibitors of various targets associated with AD, showing promising results against hAChE, hBuChE, GSK-3β, tau protein, and Aβ aggregation.
- - Compounds 6c and 6h demonstrated superior efficacy compared to the well-known AD medication donepezil, had low cytotoxicity, complied with pharmacokinetic rules, and showed potential for crossing the blood
Design and synthesis of three novel series of aryl enaminones (- and -) and pyrazole () linked compounds with sulphonamides, sulfaguanidine, or carboxylic acid functionalities were reported as carbonic anhydrase inhibitors (CAIs) using the "tail approach" strategy in their design to achieve the most variable amino acids in the middle/outer rims of the hCAs active site. The synthesised compounds were assessed for their inhibitory activity against the following human (h) isoforms, hCA I, II, IX, and XII using stopped-flow CO hydrase assay. Enaminone sulphonamide derivatives (-) potently inhibited the target tumour-associated isoforms hCA IX and hCA XII (KIs 26.
View Article and Find Full Text PDFArylidine extensions of 3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-benzenesulfonamide derivatives: Synthesis, computational simulations and biological evaluation as tumor-associated carbonic anhydrase inhibitors.
Bioorg Chem
June 2023
Several pyrazole-benzene sulfonamides were reported as human carbonic anhydrase inhibitors. In this research work, a design of Arylidine-extented 5-oxo-pyrazole benzenesulfonamides (4a-i), (8a-d) and (10a-e) were reported based on tail-approach design. Beside the reported synthetic procedures and confirmation by different analytical procedures, a DFT study was employed to confirm the Z- conformer of the synthesized compounds.
View Article and Find Full Text PDFAim: Discovery of novel series of colchicine binding site inhibitors (CBSIs).
Materials & Methods: Isoxazoline 3a-d, pyrazoline 4a-b, 7a-f and 8a-f, cyclohexenone 9a-b and 10a-b or pyridine derivatives 11a-b were synthesized and evaluated for their inhibition of tubulin polymerization and cytotoxicity. Most of the compounds displayed potent to moderate antitumor activity against leukemia SR cell line.