Literature DB >> 25616902

Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors.

Bin Wu1, Hui-Ling Wang2, Victor J Cee2, Brian A Lanman2, Thomas Nixey2, Liping Pettus2, Anthony B Reed2, Ryan P Wurz2, Nadia Guerrero3, Christine Sastri3, Jeff Winston3, J Russell Lipford3, Matthew R Lee4, Christopher Mohr4, Kristin L Andrews4, Andrew S Tasker2.   

Abstract

PIM kinases are a family of Ser/Thr kinases that are implicated in tumorigenesis. The discovery of a new class of PIM inhibitors, 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines, is discussed with optimized compounds showing excellent potency against all three PIM isoforms.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  1,3,4-Thiadiazol-2-amines; Kinase inhibitors; Lead optimization; PIM kinases

Mesh：

Substances：

Year:  2015        PMID： 25616902     DOI： 10.1016/j.bmcl.2014.12.091

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

1.  From fighting depression to conquering tumors: a novel tricyclic thiazepine compound as a tubulin polymerization inhibitor.

Authors:  Y Mu; Y Liu; J Xiang; Q Zhang; S Zhai; D P Russo; H Zhu; X Bai; B Yan
Journal:  Cell Death Dis       Date:  2016-03-17       Impact factor: 8.469

2.  QSAR studies on PIM1 and PIM2 inhibitors using statistical methods: a rustic strategy to screen for 5-(1H-indol-5-yl)-1,3,4-thiadiazol analogues and predict their PIM inhibitory activity.

Authors:  Adnane Aouidate; Adib Ghaleb; Mounir Ghamali; Samir Chtita; M'barek Choukrad; Abdelouahid Sbai; Mohammed Bouachrine; Tahar Lakhlifi
Journal:  Chem Cent J       Date:  2017-05-19       Impact factor: 4.215

3.  QSAR study and rustic ligand-based virtual screening in a search for aminooxadiazole derivatives as PIM1 inhibitors.

Authors:  Adnane Aouidate; Adib Ghaleb; Mounir Ghamali; Samir Chtita; Abdellah Ousaa; M'barek Choukrad; Abdelouahid Sbai; Mohammed Bouachrine; Tahar Lakhlifi
Journal:  Chem Cent J       Date:  2018-03-22       Impact factor: 4.215
  3 in total

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