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Your search keyword '"Mohamed N. El-Bayaa"' showing total 2 results
Start Over Author "Mohamed N. El-Bayaa" Topic mcf-7
2 results on '"Mohamed N. El-Bayaa"'

1. Synthesis and Cytotoxic Activity of New 1,3,4-Thiadiazole Thioglycosides and 1,2,3-Triazolyl-1,3,4-Thiadiazole N-glycosides

Author

Fahad M. Alminderej, Hussein H. Elganzory, Mohamed N. El-Bayaa, Hanem M. Awad, and Wael A. El-Sayed

Subjects
click chemistry, 1,3,4-thiadiazoles, 1,2,3-triazoles, glycosides, cytotoxic, hct-116, mcf-7, Organic chemistry, QD241-441
Abstract

New 1,3,4-thiadiazole thioglycosides linked to substituted arylidine systems were synthesized via glycosylation of the prepared 1,3,4-thiadiazole thiol compounds. Click strategy was also used for the synthesis of new 1,3,4-thiadiazole and 1,2,3-triazole hybrid glycosides by reaction of the acetylenic derivatives with different glycosyl azids followed by deacetylation process. The cytotoxic activities of the prepared compounds were studied against HCT-116 (human colorectal carcinoma) and MCF-7 (human breast adenocarcinoma) cell lines using the MTT assay. The results showed that the key thiadiazolethione compounds 2 and 3, the triazole glycosides linked to p-methoxyarylidine derivatives 14 and 15 in addition to the free hydroxyl glycoside 20 were found potent in activity comparable to the reference drug doxorubicin against MCF-7 human cancer cells. The acetylenic derivative 2 and glycoside 20 were also found highly active against HCT-116 cell lines.

Published
2019
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2. Design, Synthesis, Anticancer Activity and Molecular Docking of New 1,2,3-Triazole-Based Glycosides Bearing 1,3,4-Thiadiazolyl, Indolyl and Arylacetamide Scaffolds

Author

Hussein H. Elganzory, Fahad M. Alminderej, Mohamed N. El-Bayaa, Hanem M. Awad, Eman S. Nossier, and Wael A. El-Sayed

Subjects
Azides, Molecular Structure, Organic Chemistry, Pharmaceutical Science, Antineoplastic Agents, Triazoles, Analytical Chemistry, Molecular Docking Simulation, ErbB Receptors, Structure-Activity Relationship, Thioglycosides, Doxorubicin, Chemistry (miscellaneous), Alkynes, Drug Discovery, MCF-7 Cells, Humans, Molecular Medicine, Glycosides, Drug Screening Assays, Antitumor, Physical and Theoretical Chemistry, triazole, indole, glycosides, thiadiazole, arylacetamide, EGFR, HCT-116, MCF-7, anticancer, Cell Proliferation
Abstract

New 1,3,4-thiadiazole thioglycosides linked to a substituted arylidine system were synthesized via heterocyclization via click 1,3-dipolar cycloaddition. The click strategy was used for the synthesis of new 1,3,4-thiadiazole and 1,2,3-triazole hybrid glycoside-based indolyl systems as novel hybrid molecules by reacting azide derivatives with the corresponding acetylated glycosyl terminal acetylenes. The cytotoxic activities of the compounds were studied against HCT-116 (human colorectal carcinoma) and MCF-7 (human breast adenocarcinoma) cell lines using the MTT assay. The results showed that the key thiadiazolethione compounds, the triazole glycosides linked to p-methoxyarylidine derivatives and the free hydroxyl glycoside had potent activity comparable to the reference drug, doxorubicin, against MCF-7 human cancer cells. Docking simulation studies were performed to check the binding patterns of the synthesized compounds. Enzyme inhibition assay studies were also conducted for the epidermal growth factor receptor (EGFR), and the results explained the activity of a number of derivatives.

Published
2022
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