2021
Němec, Václav; Maier, Lukáš; Berger, Benedict-Tilman; Chaikuad, Apirat; Drápela, Stanislav; Souček, Karel; Knapp, Stefan; Paruch, Kamil
Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core. Journal Article
In: European journal of medicinal chemistry, vol. 215, pp. 113299, 2021, ISSN: 1768-3254 0223-5234, (Place: France).
Abstract | Links | BibTeX | Tags: 2-b]pyridine, Animals, Carrier Proteins/*antagonists & inhibitors/metabolism, CLK, Crystallography, Furans/chemical synthesis/metabolism/*pharmacology, Furo[3, HIPK, Humans, Inhibitor, Kinase, MCF-7 Cells, Mice, Molecular Structure, MU1210, MU135, MU1787, Protein Binding, Protein Kinase Inhibitors/chemical synthesis/metabolism/*pharmacology, Protein Serine-Threonine Kinases/*antagonists & inhibitors/metabolism, Pyridines/chemical synthesis/metabolism/*pharmacology, Structure-Activity Relationship, X-Ray
@article{nemec_highly_2021,
title = {Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core.},
author = {Václav Němec and Lukáš Maier and Benedict-Tilman Berger and Apirat Chaikuad and Stanislav Drápela and Karel Souček and Stefan Knapp and Kamil Paruch},
doi = {10.1016/j.ejmech.2021.113299},
issn = {1768-3254 0223-5234},
year = {2021},
date = {2021-04-01},
journal = {European journal of medicinal chemistry},
volume = {215},
pages = {113299},
abstract = {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.},
note = {Place: France},
keywords = {2-b]pyridine, Animals, Carrier Proteins/*antagonists & inhibitors/metabolism, CLK, Crystallography, Furans/chemical synthesis/metabolism/*pharmacology, Furo[3, HIPK, Humans, Inhibitor, Kinase, MCF-7 Cells, Mice, Molecular Structure, MU1210, MU135, MU1787, Protein Binding, Protein Kinase Inhibitors/chemical synthesis/metabolism/*pharmacology, Protein Serine-Threonine Kinases/*antagonists & inhibitors/metabolism, Pyridines/chemical synthesis/metabolism/*pharmacology, Structure-Activity Relationship, X-Ray},
pubstate = {published},
tppubtype = {article}
}