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

[ Vol. 18 , Issue. 2 ]

Author(s):

Rania Helmy Abd El-Hameed, Samar Said Fatahala* and Amira Ibrahim Sayed   Pages 238 - 248 ( 11 )

Abstract:


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.

Affiliation:

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan, Cairo, Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan, Cairo, Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan, Cairo



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