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Benzimidazole derivatives protect against cytokine-induced apoptosis in pancreatic β-Cells.

Abstract：

:Apoptotic cell death is the cause of the loss of insulin-producing β-cells in all forms of diabetes mellitus. The identification of small molecules capable of protecting cytokine-induced apoptosis could form the basis of useful therapeutic interventions. Here in, we present the discovery and synthesis of new benzimidazole derivatives, capable of rescuing pancreatic β-cells from cytokine-induced apoptosis. Three hydrazone derivatives of benzimidazole significantly increased the cellular ATP levels, reduced caspase-3 activity, reduced nitrite production and increased glucose-stimulated insulin secretion in the presence of proinflammatory cytokines. These findings suggest that these compounds may protect β-cells from the harmful effects of cytokines and may serve as candidates for therapeutic intervention for diabetes.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zawawi NK,Rajput SA,Taha M,Ahmat N,Ismail NH,Abdullah N,Khan KM,Choudhary MI

doi

10.1016/j.bmcl.2015.08.022

subject

Has Abstract

pub_date

2015-10-15 00:00:00

pages

4672-6

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)00857-4

journal_volume

25

pub_type

杂志文章

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