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Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F21%3A00542177" target="_blank" >RIV/68081707:_____/21:00542177 - isvavai.cz</a>

  • Alternative codes found

    RIV/00159816:_____/21:00075200 RIV/00216224:14310/21:00121502

  • Result on the web

    <a href="https://www.sciencedirect.com/science/article/pii/S0223523421001483?via%3Dihub" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0223523421001483?via%3Dihub</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1016/j.ejmech.2021.113299" target="_blank" >10.1016/j.ejmech.2021.113299</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core

  • Original language description

    The furo [3,2-b]pyridine motif represents a relatively underexplored central pharmacophore in the area of kinase inhibitors. Herein, we report flexible synthesis of 3,5-disubstituted furo [3,2-b]pyridines that relies on chemoselective couplings of newly prepared 5-chloro-3-iodofuro [3,2-b]pyridine. This methodology allowed efficient second-generation synthesis of the state-of-the-art chemical biology probe for CLK1/2/4 MU1210, and identification of the highly selective inhibitors of HIPKs MU135 and MU1787 which are presented and characterized in this study, including the X-ray crystal structure of MU135 in HIPK2. chemical biology probe (c) 2021 Published by Elsevier Masson SAS.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    30104 - Pharmacology and pharmacy

Result continuities

  • Project

    Result was created during the realization of more than one project. More information in the Projects tab.

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2021

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    European Journal of Medicinal Chemistry

  • ISSN

    0223-5234

  • e-ISSN

    1768-3254

  • Volume of the periodical

    215

  • Issue of the periodical within the volume

    APR 5 2021

  • Country of publishing house

    FR - FRANCE

  • Number of pages

    8

  • Pages from-to

    113299

  • UT code for WoS article

    000634820600034

  • EID of the result in the Scopus database

    2-s2.0-85101416586