Literature DB >> 20172718

Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing.

Pascal Furet1, Marc Gerspacher, Carole Pissot-Soldermann.   

Abstract

JAK2 is a target of high interest in chronic myeloproliferative disorders drug research. Starting from a screening hit, two new JAK2 inhibitor chemotypes were designed by scaffold morphing. The prototype compounds of these new series showed nanomolar inhibition of the kinase. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20172718     DOI: 10.1016/j.bmcl.2010.01.151

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


  3 in total

Review 1.  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

2.  Synthesis of Pyrrolo[1,2-a]pyrimidine Enantiomers via Domino Ring-Closure followed by Retro Diels-Alder Protocol.

Authors:  Beáta Fekete; Márta Palkó; Matti Haukka; Ferenc Fülöp
Journal:  Molecules       Date:  2017-04-13       Impact factor: 4.411

3.  Discovery of JAK2/3 Inhibitors from Quinoxalinone-Containing Compounds.

Authors:  Kamonpan Sanachai; Panupong Mahalapbutr; Lueacha Tabtimmai; Supaphorn Seetaha; Tanakorn Kittikool; Sirilata Yotphan; Kiattawee Choowongkomon; Thanyada Rungrotmongkol
Journal:  ACS Omega       Date:  2022-09-07
  3 in total

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