Bioorganic and Medicinal Chemistry, volume 34, pages 116015
Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model
1
Watarase Research Center, Discovery Research Headquarters, Kyorin Pharmaceutical Co., Ltd., 1848, Nogi, Nogi-machi, Shimotsuga-gun, Tochigi 329-0114, Japan.
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Publication type: Journal Article
Publication date: 2021-03-01
Journal:
Bioorganic and Medicinal Chemistry
Quartile SCImago
Q2
Quartile WOS
Q1
Impact factor: 3.5
ISSN: 09680896, 14643391
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
Bromodomain and extra-terminal domain (BET) protein plays an important role in epigenetic regulation, and the regulation of disruption contributes to the pathogenesis of cancer and inflammatory disease. With the goal of discovering novel BET inhibitors, especially BRD4 inhibitors, we designed and synthesized several compounds starting from our previously reported pyrido-benzodiazepinone derivative 4 to enhance BRD4 inhibitory activity while avoiding hERG inhibition. Molecular docking studies and structure-activity relationship studies led to the identification of 9-fluorobenzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivative 43, which exhibited potent BRD4 inhibitory activity with excellent potency in imiquimod-induced psoriasis model mice.
Top-30
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Russian Chemical Reviews
1 publication, 33.33%
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Citations by publishers
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Elsevier
1 publication, 33.33%
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Frontiers Media S.A.
1 publication, 33.33%
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Autonomous Non-profit Organization Editorial Board of the journal Uspekhi Khimii
1 publication, 33.33%
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- We do not take into account publications without a DOI.
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Sato M. et al. Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model // Bioorganic and Medicinal Chemistry. 2021. Vol. 34. p. 116015.
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Sato M., Kondo T., Kohno Y., SETO S. Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model // Bioorganic and Medicinal Chemistry. 2021. Vol. 34. p. 116015.
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TY - JOUR
DO - 10.1016/j.bmc.2021.116015
UR - https://doi.org/10.1016/j.bmc.2021.116015
TI - Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model
T2 - Bioorganic and Medicinal Chemistry
AU - Sato, Masanori
AU - Kondo, Takekazu
AU - Kohno, Yasushi
AU - SETO, Shigeki
PY - 2021
DA - 2021/03/01 00:00:00
PB - Elsevier
SP - 116015
VL - 34
SN - 0968-0896
SN - 1464-3391
ER -
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@article{2021_Sato,
author = {Masanori Sato and Takekazu Kondo and Yasushi Kohno and Shigeki SETO},
title = {Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model},
journal = {Bioorganic and Medicinal Chemistry},
year = {2021},
volume = {34},
publisher = {Elsevier},
month = {mar},
url = {https://doi.org/10.1016/j.bmc.2021.116015},
pages = {116015},
doi = {10.1016/j.bmc.2021.116015}
}