Literature DB >> 26320619

Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).

Qingjie Liu1, Douglas G Batt2, Jonathan S Lippy2, Neha Surti2, Andrew J Tebben2, Jodi K Muckelbauer2, Lin Chen2, Yongmi An2, Chiehying Chang2, Matt Pokross2, Zheng Yang2, Haiqing Wang2, James R Burke2, Percy H Carter2, Joseph A Tino2.   

Abstract

Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton's tyrosine kinase (BTK). 4,7- and 4,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of BTK, while 3,7- and 3,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of Janus kinase 2 (JAK2).
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Bruton’s tyrosine kinase (BTK); Carbazole; Janus kinase 2 (JAK2)

Mesh:

Substances:

Year:  2015        PMID: 26320619     DOI: 10.1016/j.bmcl.2015.07.102

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


  5 in total

1.  Pharmacophore modeling and virtual screening in search of novel Bruton's tyrosine kinase inhibitors.

Authors:  Aditya Sharma; B K Thelma
Journal:  J Mol Model       Date:  2019-06-06       Impact factor: 1.810

Review 2.  Evaluation of small molecule kinase inhibitors as novel antimicrobial and antibiofilm agents.

Authors:  Ashley King; Meghan S Blackledge
Journal:  Chem Biol Drug Des       Date:  2021-10-04       Impact factor: 2.817

3.  Receptor-guided 3D-QSAR studies, molecular dynamics simulation and free energy calculations of Btk kinase inhibitors.

Authors:  Pavithra K Balasubramanian; Anand Balupuri; Hee-Young Kang; Seung Joo Cho
Journal:  BMC Syst Biol       Date:  2017-03-14

4.  Molecular Modeling Studies on Carbazole Carboxamide Based BTK Inhibitors Using Docking and Structure-Based 3D-QSAR.

Authors:  Rui Li; Yongli Du; Zhipei Gao; Jingkang Shen
Journal:  Int J Mol Sci       Date:  2018-04-19       Impact factor: 5.923

Review 5.  The Development of BTK Inhibitors: A Five-Year Update.

Authors:  Bruno Tasso; Andrea Spallarossa; Eleonora Russo; Chiara Brullo
Journal:  Molecules       Date:  2021-12-06       Impact factor: 4.411

  5 in total

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