Literature DB >> 15125964

The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase.

Mark T Bilodeau1, Leonard D Rodman, Georgia B McGaughey, Kathleen E Coll, Timothy J Koester, William F Hoffman, Randall W Hungate, Richard L Kendall, Rosemary C McFall, Keith W Rickert, Ruth Z Rutledge, Kenneth A Thomas.   

Abstract

An azo-dye lead was modified to a novel N-(1,3-thiazol-2-yl)pyridin-2-amine series of KDR kinase inhibitors through the use of rapid analog libraries. This new class has been found to be potent, selective, and of low molecular weight. Molecular modeling has postulated an interesting conformational preference and binding mode for these compounds in the active site of the enzyme.

Entities:  

Mesh:

Substances:

Year:  2004        PMID: 15125964     DOI: 10.1016/j.bmcl.2004.03.052

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


  5 in total

1.  Scoring of KDR kinase inhibitors: using interaction energy as a guide for ranking.

Authors:  Georgia B McGaughey; J Chris Culberson; Bradley P Feuston; Constantine Kreatsoulas; Vladimir Maiorov; Joseph Shpungin
Journal:  Mol Divers       Date:  2006-09-27       Impact factor: 2.943

2.  Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.

Authors:  Hwan Geun Choi; Jianming Zhang; Ellen Weisberg; James D Griffin; Taebo Sim; Nathanael S Gray
Journal:  Bioorg Med Chem Lett       Date:  2012-06-23       Impact factor: 2.823

3.  Novel 2-(5-Aryl-4,5-Dihydropyrazol-1-yl)thiazol-4-One as EGFR Inhibitors: Synthesis, Biological Assessment and Molecular Docking Insights.

Authors:  Tarfah Al-Warhi; Ahmed M El Kerdawy; Mohamed A Said; Amgad Albohy; Zainab M Elsayed; Nada Aljaeed; Eslam B Elkaeed; Wagdy M Eldehna; Hatem A Abdel-Aziz; Miral A Abdelmoaz
Journal:  Drug Des Devel Ther       Date:  2022-05-16       Impact factor: 4.319

4.  Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign.

Authors:  Nello Mainolfi; Rajeshri Karki; Fang Liu; Karen Anderson
Journal:  ACS Med Chem Lett       Date:  2016-02-02       Impact factor: 4.345

5.  Ab-initio and Conformational Analysis of a Potent VEGFR-2 Inhibitor: A Case Study on Motesanib.

Authors:  Ahmad Ebadi; Nima Razzaghi-Asl; Sara Shahabipour; Ramin Miri
Journal:  Iran J Pharm Res       Date:  2014       Impact factor: 1.696

  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.