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Development of Isatin-Based Schiff Bases Targeting VEGFR-2 Inhibition: Synthesis, Characterization, Antiproliferative Properties, and QSAR Studies
Faculty
Pharmacy
Year:
2022
Type of Publication:
ZU Hosted
Pages:
Authors:
Israa Abdallah Mostafa Sliem
Staff Zu Site
Abstract In Staff Site
Journal:
ChemMedChem Wiley
Volume:
Keywords :
Development , Isatin-Based Schiff Bases Targeting VEGFR-2
Abstract:
Three sets of isatin-based Schiff bases were synthesized utilizing the molecular hybridization approach. Some of the synthesized Schiff bases show significant to moderate antiproliferative properties against MCF7 (breast), HCT116 (colon), and PaCa2 (pancreatic) cancer cell lines with potency compared to reference drugs 5-fluorouracil (5-FU) and Sunitinib. Among all, compound 17 f (3-((1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)imino)-1-((1-(2-methoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)-5-methylindolin-2-one) exhibits promising antiproliferative properties against the MCF7 cancer cell line with 2.1-fold more potency than Sunitinib. However, among all the synthesized compounds, three (5-methylisatin derivatives) were the most effective against HCT116 in comparison to 5-FU. Compound 17 f exhibited the highest anti-angiogenic effect on the vasculature as it significantly reduced BV from 43 mm to 2 mm in comparison to 5.7 mm for Sunitinib and flow cytometry supports the arrest of the cell cycle at G1/S phases. In addition, compound 17 f also showed high VEGFR-2 inhibition properties against breast cancer cell lines. Robust 2D-QSAR studies supported the biological data.
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Department Related Publications
Etedaal Hassan Mohamed Abdulaal, "18. In situ annelation of enaminones by reaction with methyleneiminium intermediates", لايوجد, 1900
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Hanan Abdelraziek Abdelfattah Ali Hamied, "synthesis of some new imidazolones of expected antimicrobial activity", لايوجد, 1900
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Azza Mohamed Kadry , "35. Synthesis and potentiometric study of some dioxadiaza ionophores in ion selective electrodes", لايوجد, 1900
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Azza Mohamed Kadry , "16. Chemistry of quinazolines: Reinvestigation of the action of hydrazine on thioxo derivatives", لايوجد, 1900
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Azza Mohamed Kadry , "2. Reaction and rearrangement of 2,4-quinazolinediones", لايوجد, 1900
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