Literature DB >> 19762238

Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).

Christopher J Burns1, David G Bourke, Laura Andrau, Xianyong Bu, Susan A Charman, Andrew C Donohue, Emmanuelle Fantino, Michelle Farrugia, John T Feutrill, Max Joffe, Marcel R Kling, Margarita Kurek, Tracy L Nero, Thao Nguyen, James T Palmer, Ian Phillips, David M Shackleford, Harrison Sikanyika, Michelle Styles, Stephen Su, Herbert Treutlein, Jun Zeng, Andrew F Wilks.   

Abstract

A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide). Details of synthesis and SAR studies of these compounds are reported.

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Year:  2009        PMID: 19762238     DOI: 10.1016/j.bmcl.2009.08.071

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


  16 in total

1.  Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors.

Authors:  Romain Noël; Youseung Shin; Xinyi Song; Yuanjun He; Marcel Koenig; Weimin Chen; Yuan Yuan Ling; Li Lin; Claudia H Ruiz; Phil LoGrasso; Michael D Cameron; Derek R Duckett; Theodore M Kamenecka
Journal:  Bioorg Med Chem Lett       Date:  2010-12-01       Impact factor: 2.823

2.  Molecular dynamics and integrated pharmacophore-based identification of dual [Formula: see text] inhibitors.

Authors:  Maninder Kaur; Pankaj Kumar Singh; Manjinder Singh; Renu Bahadur; Om Silakari
Journal:  Mol Divers       Date:  2017-11-14       Impact factor: 2.943

3.  Dual inhibitors of Janus kinase 2 and 3 (JAK2/3): designing by pharmacophore- and docking-based virtual screening approach.

Authors:  Haneesh Jasuja; Navriti Chadha; Maninder Kaur; Om Silakari
Journal:  Mol Divers       Date:  2014-01-11       Impact factor: 2.943

4.  Dialkylbiaryl Phosphines in Pd-Catalyzed Amination: A User's Guide.

Authors:  David S Surry; Stephen L Buchwald
Journal:  Chem Sci       Date:  2011       Impact factor: 9.825

Review 5.  JAK2 inhibitors: are they the solution?

Authors:  Fabio P S Santos; Srdan Verstovsek
Journal:  Clin Lymphoma Myeloma Leuk       Date:  2011-05-04

6.  Understanding the structural features of JAK2 inhibitors: a combined 3D-QSAR, DFT and molecular dynamics study.

Authors:  Sathya Babu; Santhosh Kumar Nagarajan; Thirumurthy Madhavan
Journal:  Mol Divers       Date:  2019-01-07       Impact factor: 2.943

Review 7.  The current status and the future of JAK2 inhibitors for the treatment of myeloproliferative diseases.

Authors:  Yasumichi Hitoshi; Nan Lin; Donald G Payan; Vadim Markovtsov
Journal:  Int J Hematol       Date:  2010-02-27       Impact factor: 2.490

8.  Structure-based design of oxygen-linked macrocyclic kinase inhibitors: discovery of SB1518 and SB1578, potent inhibitors of Janus kinase 2 (JAK2) and Fms-like tyrosine kinase-3 (FLT3).

Authors:  Anders Poulsen; Anthony William; Stéphanie Blanchard; Angeline Lee; Harish Nagaraj; Haishan Wang; Eeling Teo; Evelyn Tan; Kee Chuan Goh; Brian Dymock
Journal:  J Comput Aided Mol Des       Date:  2012-04-22       Impact factor: 3.686

Review 9.  The recent medicinal chemistry development of Jak2 tyrosine kinase small molecule inhibitors.

Authors:  R Baskin; A Majumder; P P Sayeski
Journal:  Curr Med Chem       Date:  2010       Impact factor: 4.530

10.  JAK1/STAT3 Activation through a Proinflammatory Cytokine Pathway Leads to Resistance to Molecularly Targeted Therapy in Non-Small Cell Lung Cancer.

Authors:  Kazuhiko Shien; Vassiliki A Papadimitrakopoulou; Dennis Ruder; Carmen Behrens; Li Shen; Neda Kalhor; Juhee Song; J Jack Lee; Jing Wang; Ximing Tang; Roy S Herbst; Shinichi Toyooka; Luc Girard; John D Minna; Jonathan M Kurie; Ignacio I Wistuba; Julie G Izzo
Journal:  Mol Cancer Ther       Date:  2017-07-20       Impact factor: 6.261

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