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://www.sciencedirect.com/science/article/pii/S...
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 |
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Source: | Copyright of this article belongs to Elsevier Science. |
Keywords: | GSK-3; CDK-2; Molecular Docking; Molecular Dynamics; SBDD |
ID Code: | 100234 |
Deposited On: | 12 Feb 2018 12:56 |
Last Modified: | 12 Feb 2018 12:56 |
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