期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 121, 期 -, 页码 727-736出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.04.075
关键词
GSK-3; CDK-2; Molecular docking; Molecular dynamics; SBDD
资金
- Department of Science and Technology (DST), Govt. of India, New Delhi, India
- NIPER, S. A. S. Nagar
- University Grant Commission (UGC), Govt. of India, New Delhi, India [43395]
In this work, iminothiazolidin-4-one derivatives were explored as selective GSK-3 beta 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. (C) 2016 Elsevier Masson SAS. All rights reserved.
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