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Your search keyword '"Elmeligie, Salwa"' showing total 4 results
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4 results on '"Elmeligie, Salwa"'

3. Design, synthesis, and biological evaluation of novel ciprofloxacin derivatives as potential anticancer agents targeting topoisomerase II enzyme

Author

Swedan, Hadeer K., Kassab, Asmaa E., Gedawy, Ehab M., and Elmeligie, Salwa E.

Subjects
Pharmacology, Molecular Structure, Dose-Response Relationship, Drug, Antineoplastic Agents, General Medicine, Molecular Docking Simulation, Structure-Activity Relationship, DNA Topoisomerases, Type II, Ciprofloxacin, Doxorubicin, Cell Line, Tumor, Drug Discovery, Drug Screening Assays, Antitumor, Cell Proliferation
Abstract

A series of novel ciprofloxacin (CP) derivatives substituted at the N-4 position with biologically active moieties were designed and synthesised. 14 compounds were 1.02- to 8.66-fold more potent than doxorubicin against T-24 cancer cells. Ten compounds were 1.2- to 7.1-fold more potent than doxorubicin against PC-3 cancer cells. The most potent compounds 6, 7a, 7b, 8a, 9a, and 10c showed significant Topo II inhibitory activity (83–90% at 100 μM concentration). Compounds 6, 8a, and 10c were 1.01- to 2.32-fold more potent than doxorubicin. Compounds 6 and 8a induced apoptosis in T-24 (16.8- and 20.1-fold, respectively compared to control). This evidence was supported by an increase in the level of apoptotic caspase-3 (5.23- and 7.6-fold, sequentially). Both compounds arrested the cell cycle in the S phase in T-24 cancer cells while in PC-3 cancer cells the two compounds arrested the cell cycle in the G1 phase. Molecular docking simulations of compounds 6 and 8a into the Topo II active site rationalised their remarkable Topo II inhibitory activity.

Published
2022

4. Design, synthesis, and biological evaluation of novel ciprofloxacin derivatives as potential anticancer agents targeting topoisomerase II enzyme.

Author

Swedan, Hadeer K., Kassab, Asmaa E., Gedawy, Ehab M., and Elmeligie, Salwa E.

Subjects
DNA topoisomerase I, DNA topoisomerase II, ANTINEOPLASTIC agents, CIPROFLOXACIN, CELL cycle, CANCER cells, MOLECULAR docking
Abstract

A series of novel ciprofloxacin (CP) derivatives substituted at the N-4 position with biologically active moieties were designed and synthesised. 14 compounds were 1.02- to 8.66-fold more potent than doxorubicin against T-24 cancer cells. Ten compounds were 1.2- to 7.1-fold more potent than doxorubicin against PC-3 cancer cells. The most potent compounds 6, 7a, 7b, 8a, 9a, and 10c showed significant Topo II inhibitory activity (83–90% at 100 μM concentration). Compounds 6, 8a, and 10c were 1.01- to 2.32-fold more potent than doxorubicin. Compounds 6 and 8a induced apoptosis in T-24 (16.8- and 20.1-fold, respectively compared to control). This evidence was supported by an increase in the level of apoptotic caspase-3 (5.23- and 7.6-fold, sequentially). Both compounds arrested the cell cycle in the S phase in T-24 cancer cells while in PC-3 cancer cells the two compounds arrested the cell cycle in the G1 phase. Molecular docking simulations of compounds 6 and 8a into the Topo II active site rationalised their remarkable Topo II inhibitory activity. [ABSTRACT FROM AUTHOR]

Published
2023
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