Literature DB >> 19071018

Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.

Stanley D Chamberlain1, Anikó M Redman, Joseph W Wilson, Felix Deanda, J Brad Shotwell, Roseanne Gerding, Huangshu Lei, Bin Yang, Kirk L Stevens, Anne M Hassell, Lisa M Shewchuk, M Anthony Leesnitzer, Jeffery L Smith, Peter Sabbatini, Charity Atkins, Arthur Groy, Jason L Rowand, Rakesh Kumar, Robert A Mook, Ganesh Moorthy, Samarjit Patnaik.   

Abstract

The SAR of C5' functional groups with terminal basic amines at the C6 aniline of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines is reported. Examples demonstrate potent inhibition of IGF-1R with 1000-fold selectivity over JNK1 and 3 in enzymatic assays.

Entities:  

Mesh：

Substances：

Year:  2008        PMID： 19071018     DOI： 10.1016/j.bmcl.2008.11.077

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


  12 in total

1.  Understanding the specificity of a docking interaction between JNK1 and the scaffolding protein JIP1.

Authors:  Chunli Yan; Tamer Kaoud; Sunbae Lee; Kevin N Dalby; Pengyu Ren
Journal:  J Phys Chem B       Date:  2011-01-25       Impact factor: 2.991

2.  Potent Pyrimidine and Pyrrolopyrimidine Inhibitors of Testis-Specific Serine/Threonine Kinase 2 (TSSK2).

Authors:  Jon E Hawkinson; Rondedrick Sinville; Deepti Mudaliar; Jagathpala Shetty; Timothy Ward; John C Herr; Gunda I Georg
Journal:  ChemMedChem       Date:  2017-10-20       Impact factor: 3.466

Review 3.  ALK and ROS1 as a joint target for the treatment of lung cancer: a review.

Authors:  Raimon Puig de la Bellacasa; Niki Karachaliou; Roger Estrada-Tejedor; Jordi Teixidó; Carlota Costa; José I Borrell
Journal:  Transl Lung Cancer Res       Date:  2013-04

4.  Enzyme kinetics and interaction studies for human JNK1β1 and substrates activating transcription factor 2 (ATF2) and c-Jun N-terminal kinase (c-Jun).

Authors:  Mariana Figuera-Losada; Philip V LoGrasso
Journal:  J Biol Chem       Date:  2012-02-17       Impact factor: 5.157

5.  Profiling MAP kinase cysteines for targeted covalent inhibitor design.

Authors:  Ruibin Liu; Neha Verma; Jack A Henderson; Shaoqi Zhan; Jana Shen
Journal:  RSC Med Chem       Date:  2021-11-03

Review 6.  Recent developments in the structural characterisation of the IR and IGF1R: implications for the design of IR-IGF1R hybrid receptor modulators.

Authors:  Samuel J Turvey; Martin J McPhillie; Mark T Kearney; Stephen P Muench; Katie J Simmons; Colin W G Fishwick
Journal:  RSC Med Chem       Date:  2022-02-21

Review 7.  Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.

Authors:  Rongshi Li; Alan Pourpak; Stephan W Morris
Journal:  J Med Chem       Date:  2009-08-27       Impact factor: 7.446

8.  A highly selective dual insulin receptor (IR)/insulin-like growth factor 1 receptor (IGF-1R) inhibitor derived from an extracellular signal-regulated kinase (ERK) inhibitor.

Authors:  Theonie Anastassiadis; Krisna C Duong-Ly; Sean W Deacon; Alec Lafontant; Haiching Ma; Karthik Devarajan; Roland L Dunbrack; Jinhua Wu; Jeffrey R Peterson
Journal:  J Biol Chem       Date:  2013-08-09       Impact factor: 5.157

9.  Analysis of conditions affecting auto-phosphorylation of human kinases during expression in bacteria.

Authors:  Amit Shrestha; Garth Hamilton; Eric O'Neill; Stefan Knapp; Jonathan M Elkins
Journal:  Protein Expr Purif       Date:  2011-10-01       Impact factor: 1.650

10.  Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors.

Authors:  Kristoff T Homan; Kelly M Larimore; Jonathan M Elkins; Marta Szklarz; Stefan Knapp; John J G Tesmer
Journal:  ACS Chem Biol       Date:  2014-10-03       Impact factor: 5.100
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.