Literature DB >> 21862328

Identification and SAR of a new series of thieno[3,2-d]pyrimidines as Tpl2 kinase inhibitors.

Yike Ni1, Ariamala Gopalsamy, Derek Cole, Yonghan Hu, Rajiah Denny, Manus Ipek, Julie Liu, Julie Lee, J Perry Hall, Michael Luong, Jean-Baptiste Telliez, Lih-Ling Lin.   

Abstract

We report here the synthesis and SAR of a new series of thieno[3,2-d]pyrimidines as potent Tpl2 kinase inhibitors. The proposed binding mode suggests the potential flipped binding mode depending on the substitution. Biacore studies show evidence of binding of these molecules to the protein kinase. The kinome inhibition profile of these molecules suggests good selectivity.
Copyright © 2011 Elsevier Ltd. All rights reserved.

Entities:  

Mesh:

Substances:

Year:  2011        PMID: 21862328     DOI: 10.1016/j.bmcl.2011.07.069

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


  5 in total

1.  Thieno[2,3-d]pyrimidinedione derivatives as antibacterial agents.

Authors:  Mahender B Dewal; Amit S Wani; Celine Vidaillac; David Oupický; Michael J Rybak; Steven M Firestine
Journal:  Eur J Med Chem       Date:  2012-02-25       Impact factor: 6.514

Review 2.  Macrophages in multiple myeloma: emerging concepts and therapeutic implications.

Authors:  Fotis Asimakopoulos; Jaehyup Kim; Ryan A Denu; Chelsea Hope; Jeffrey L Jensen; Samuel J Ollar; Ellen Hebron; Claire Flanagan; Natalie Callander; Peiman Hematti
Journal:  Leuk Lymphoma       Date:  2013-04-11

3.  A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.

Authors:  Alfredo Picado; Apirat Chaikuad; Carrow I Wells; Safal Shrestha; William J Zuercher; Julie E Pickett; Frank E Kwarcinski; Parvathi Sinha; Chandi S de Silva; Reena Zutshi; Shubin Liu; Natarajan Kannan; Stefan Knapp; David H Drewry; Timothy M Willson
Journal:  J Med Chem       Date:  2020-11-20       Impact factor: 7.446

4.  Synthesis and Antitumor Evaluation of Menthone-Derived Pyrimidine-Urea Compounds as Potential PI3K/Akt/mTOR Signaling Pathway Inhibitor.

Authors:  Mei Huang; Wengui Duan; Naiyuan Chen; Guishan Lin; Xiu Wang
Journal:  Front Chem       Date:  2022-02-03       Impact factor: 5.221

5.  Genetic and pharmacologic inhibition of Tpl2 kinase is protective in a mouse model of ventilator-induced lung injury.

Authors:  Evangelos Kaniaris; Katerina Vaporidi; Eleni Vergadi; Emmanuel E Theodorakis; Eumorfia Kondili; Eleni Lagoudaki; Christos Tsatsanis; Dimitris Georgopoulos
Journal:  Intensive Care Med Exp       Date:  2014-05-09
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.