Design, synthesis and biological evaluation of 5-benzylidene-2-iminothiazolidin-4-ones as selective GSK-3β inhibitors

Arfeen, Minhajul ; Bhagat, Shweta ; Patel, Rahul ; Prasad, Shivcharan ; Roy, Ipsita ; Chakraborti, Asit K. ; Bharatam, Prasad V. (2016) Design, synthesis and biological evaluation of 5-benzylidene-2-iminothiazolidin-4-ones as selective GSK-3β inhibitors European Journal of Medicinal Chemistry, 121 . pp. 727-736. ISSN 0223-5234

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Official URL: http://doi.org/10.1016/j.ejmech.2016.04.075

Related URL: http://dx.doi.org/10.1016/j.ejmech.2016.04.075

Abstract

In this work, iminothiazolidin-4-one derivatives were explored as selective GSK-3β inhibitors. Molecular docking analysis was carried to design a series of compounds, which were synthesized using substituted thiourea, 2-bromoacetophenones and benzaldehydes. Out of the twenty five compounds synthesized during this work, the in vitro evaluation against GSK-3 led to the identification of nine compounds with activity in lower nano-molar range (2-85 nM). Further, in vitro evaluation against CDK-2 showed five compounds to be selective towards GSK-3.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:CDK-2; GSK-3; Molecular Docking; Molecular Dynamics; SBDD.
ID Code:116376
Deposited On:12 Apr 2021 09:28
Last Modified:12 Apr 2021 09:28

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