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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Research Article

Synthesis of Some Novel Benzimidazole Derivatives as Anticancer Agent and Evaluation for CDK2 Inhibition Activity

Author(s): Rania Helmy Abd El-Hameed, Samar Said Fatahala* and Amira Ibrahim Sayed

Volume 18 , Issue 2 , 2022

Published on: 04 March, 2021

Page: [238 - 248] Pages: 11

DOI: 10.2174/1573406417666210304100830

Price: $65


Background: Thiobezimidazoles reveal various pharmacological activities due to similarities with many natural and synthetic molecules; they can easily interact with biomolecules of living systems.

Objective: A series of substituted 2-thiobezimidazoles have been synthesized. Twelve final compounds were screened for in vitro anti-cancer activities against sixty different cell lines.

Methods: The spectral data of the synthesized compounds were characterized. A docking study for active anticancer compounds and CDK2/CyclinA2 Kinase assay against standard reference; Imatinib, were performed.

Results: Two compounds (3c&3l) from the examined series revealed effective antitumor activity in vitro against two-cancer cell lines (Colon Cancer (HCT-116) and Renal Cancer (TK-10). The docking study of synthesized molecules discovered a requisite binding pose in the CDK-ATP binding pocket .3c &3l were promoted in the CDK2/CyclinA2 Kinase assay against standard reference Imatinib.

Conclusion: Against all tested compounds; two compounds 3c &3l were found active against two types of cell-lines.

Keywords: Anti-cancer, Synthesis, 2-thiobenzimidazoles, spectroscopic analysis, docking, CDK2 assay.

Graphical Abstract
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