8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors
Тип публикации: Journal Article
Дата публикации: 2016-01-07
SCImago Q1
Tоп 10% SCImago
WOS Q1
БС1
SJR: 1.726
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
26741168
Drug Discovery
Molecular Medicine
Краткое описание
We report the discovery of N-substituted 4-(pyridin-2-yl)thiazole-2-amine derivatives and their subsequent optimization, guided by structure-based design, to give 8-(1H-pyrazol-3-yl)pyrido[3,4-d]pyrimidin-4(3H)-ones, a series of potent JmjC histone N-methyl lysine demethylase (KDM) inhibitors which bind to Fe(II) in the active site. Substitution from C4 of the pyrazole moiety allows access to the histone peptide substrate binding site; incorporation of a conformationally constrained 4-phenylpiperidine linker gives derivatives such as 54j and 54k which demonstrate equipotent activity versus the KDM4 (JMJD2) and KDM5 (JARID1) subfamily demethylases, selectivity over representative exemplars of the KDM2, KDM3, and KDM6 subfamilies, cellular permeability in the Caco-2 assay, and, for 54k, inhibition of H3K9Me3 and H3K4Me3 demethylation in a cell-based assay.
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Bavetsias V. et al. 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors // Journal of Medicinal Chemistry. 2016. Vol. 59. No. 4. pp. 1388-1409.
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Bavetsias V. et al. 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors // Journal of Medicinal Chemistry. 2016. Vol. 59. No. 4. pp. 1388-1409.
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TY - JOUR
DO - 10.1021/acs.jmedchem.5b01635
UR - https://doi.org/10.1021/acs.jmedchem.5b01635
TI - 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors
T2 - Journal of Medicinal Chemistry
AU - Bavetsias, Vassilios
AU - Lanigan, Rachel M
AU - Ruda, Gian Filippo
AU - Atrash, Butrus
AU - Mclaughlin, Mark
AU - Tumber, Anthony
AU - Mok, N Yi
AU - Le Bihan, Yann-Vaï
AU - Dempster, Sally
AU - Boxall, Katherine J
AU - Jeganathan, Fiona
AU - Hatch, Stephanie B
AU - Savitsky, Pavel
AU - Srikannathasan, Velupillai
AU - Krojer, Tobias
AU - England, Katherine S
AU - Sejberg, Jimmy
AU - Thai, Ching
AU - Donovan, Adam
AU - Pal, Akos
AU - Scozzafava, Giuseppe
AU - Bennett, James M
AU - Kawamura, Akane
AU - Johansson, Catrine
AU - Szykowska, Aleksandra
AU - Gileadi, Carina
AU - Burgess-Brown, Nicola A.
AU - von Delft, Frank
AU - Oppermann, Udo C.I.
AU - Walters, Zoë S
AU - Shipley, Janet
AU - Raynaud, F.
AU - Westaway, Susan M.
AU - Prinjha, Rab K
AU - Fedorov, Oleg
AU - Burke, Rosemary
AU - Schofield, Christopher J.
AU - WESTWOOD, Isaac M.
AU - Bountra, C
AU - Müller, Susanne
AU - van Montfort, Rob L. M.
AU - Brennan, Paul M.
AU - Blagg, J.
PY - 2016
DA - 2016/01/07
PB - American Chemical Society (ACS)
SP - 1388-1409
IS - 4
VL - 59
PMID - 26741168
SN - 0022-2623
SN - 1520-4804
ER -
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@article{2016_Bavetsias,
author = {Vassilios Bavetsias and Rachel M Lanigan and Gian Filippo Ruda and Butrus Atrash and Mark Mclaughlin and Anthony Tumber and N Yi Mok and Yann-Vaï Le Bihan and Sally Dempster and Katherine J Boxall and Fiona Jeganathan and Stephanie B Hatch and Pavel Savitsky and Velupillai Srikannathasan and Tobias Krojer and Katherine S England and Jimmy Sejberg and Ching Thai and Adam Donovan and Akos Pal and Giuseppe Scozzafava and James M Bennett and Akane Kawamura and Catrine Johansson and Aleksandra Szykowska and Carina Gileadi and Nicola A. Burgess-Brown and Frank von Delft and Udo C.I. Oppermann and Zoë S Walters and Janet Shipley and F. Raynaud and Susan M. Westaway and Rab K Prinjha and Oleg Fedorov and Rosemary Burke and Christopher J. Schofield and Isaac M. WESTWOOD and C Bountra and Susanne Müller and Rob L. M. van Montfort and Paul M. Brennan and J. Blagg and others},
title = {8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors},
journal = {Journal of Medicinal Chemistry},
year = {2016},
volume = {59},
publisher = {American Chemical Society (ACS)},
month = {jan},
url = {https://doi.org/10.1021/acs.jmedchem.5b01635},
number = {4},
pages = {1388--1409},
doi = {10.1021/acs.jmedchem.5b01635}
}
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Bavetsias, Vassilios, et al. “8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.” Journal of Medicinal Chemistry, vol. 59, no. 4, Jan. 2016, pp. 1388-1409. https://doi.org/10.1021/acs.jmedchem.5b01635.
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