Literature DB >> 18755587

Discovery of thieno[2,3-c]pyridines as potent COT inhibitors.

Dawn George1, Michael Friedman, Hamish Allen, Maria Argiriadi, Claude Barberis, Agnieszka Bischoff, Anca Clabbers, Kevin Cusack, Richard Dixon, Shannon Fix-Stenzel, Thomas Gordon, Bernd Janssen, Yong Jia, Maria Moskey, Christopher Quinn, Jose-Andres Salmeron, Neil Wishart, Kevin Woller, Zhengtian Yu.   

Abstract

Evaluation of hit chemotypes from high throughput screening identified a novel series of 2,4-disubstituted thieno[2,3-c]pyridines as COT kinase inhibitors. Structural modifications exploring SAR at the 2- and 4-positions resulting in inhibitors with improved enzyme potency and cellular activity are disclosed.

Entities:  

Mesh：

Substances：

Year:  2008        PMID： 18755587     DOI： 10.1016/j.bmcl.2008.08.037

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


  9 in total

Review 1.  Targeting innate immunity protein kinase signalling in inflammation.

Authors:  Matthias Gaestel; Alexey Kotlyarov; Michael Kracht
Journal:  Nat Rev Drug Discov       Date:  2009-06       Impact factor: 84.694

Review 2.  In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases.

Authors:  C I Wells; N R Kapadia; R M Couñago; D H Drewry
Journal:  Medchemcomm       Date:  2017-12-08       Impact factor: 3.597

3.  Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.

Authors:  Michael F T Koehler; Philippe Bergeron; Elizabeth M Blackwood; Krista Bowman; Kevin R Clark; Ron Firestein; James R Kiefer; Klaus Maskos; Mark L McCleland; Linda Orren; Laurent Salphati; Steve Schmidt; Elisabeth V Schneider; Jiansheng Wu; Maureen H Beresini
Journal:  ACS Med Chem Lett       Date:  2016-01-06       Impact factor: 4.345

4.  Cot/tpl2 (MAP3K8) mediates myeloperoxidase activity and hypernociception following peripheral inflammation.

Authors:  Irene Soria-Castro; Agnieszka Krzyzanowska; Marta López Pelaéz; Javier Regadera; Gema Ferrer; Lluis Montoliu; Rosario Rodríguez-Ramos; Margarita Fernández; Susana Alemany
Journal:  J Biol Chem       Date:  2010-08-24       Impact factor: 5.157

5.  The Crystal Structure of Cancer Osaka Thyroid Kinase Reveals an Unexpected Kinase Domain Fold.

Authors:  Sascha Gutmann; Alexandra Hinniger; Gabriele Fendrich; Peter Drückes; Sylvie Antz; Henri Mattes; Henrik Möbitz; Silvio Ofner; Niko Schmiedeberg; Aleksandar Stojanovic; Sebastien Rieffel; André Strauss; Thomas Troxler; Ralf Glatthar; Helmut Sparrer
Journal:  J Biol Chem       Date:  2015-04-27       Impact factor: 5.157

Review 6.  Regulation and function of TPL-2, an IκB kinase-regulated MAP kinase kinase kinase.

Authors:  Thorsten Gantke; Srividya Sriskantharajah; Steven C Ley
Journal:  Cell Res       Date:  2010-12-07       Impact factor: 25.617

7.  COT drives resistance to RAF inhibition through MAP kinase pathway reactivation.

Authors:  Cory M Johannessen; Jesse S Boehm; So Young Kim; Sapana R Thomas; Leslie Wardwell; Laura A Johnson; Caroline M Emery; Nicolas Stransky; Alexandria P Cogdill; Jordi Barretina; Giordano Caponigro; Haley Hieronymus; Ryan R Murray; Kourosh Salehi-Ashtiani; David E Hill; Marc Vidal; Jean J Zhao; Xiaoping Yang; Ozan Alkan; Sungjoon Kim; Jennifer L Harris; Christopher J Wilson; Vic E Myer; Peter M Finan; David E Root; Thomas M Roberts; Todd Golub; Keith T Flaherty; Reinhard Dummer; Barbara L Weber; William R Sellers; Robert Schlegel; Jennifer A Wargo; William C Hahn; Levi A Garraway
Journal:  Nature       Date:  2010-11-24       Impact factor: 49.962

8.  Assaying kinase activity of the TPL-2/NF-κB1 p105/ABIN-2 complex using an optimal peptide substrate.

Authors:  Sandra Kümper; Thorsten Gantke; Chao-Sheng Chen; Yasmina Soneji; Michael J Pattison; Probir Chakravarty; Svend Kjær; Daniel Thomas; Carl Haslam; Bill J Leavens; David House; David J Powell; Steven C Ley
Journal:  Biochem J       Date:  2018-01-11       Impact factor: 3.857

9.  Structure-Activity Relationship (SAR) Study of Spautin-1 to Entail the Discovery of Novel NEK4 Inhibitors.

Authors:  Mathias Elsocht; Philippe Giron; Laila Maes; Wim Versées; Gustavo J Gutierrez; Jacques De Grève; Steven Ballet
Journal:  Int J Mol Sci       Date:  2021-01-10       Impact factor: 5.923
  9 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.