Ring size changes in the development of class I HDAC inhibitors

Er Chieh Cho; Chi Yuan Liu; Di Wei Tang; Hsueh Yun Lee

doi:10.1080/14756366.2021.1941920

Ring size changes in the development of class I HDAC inhibitors

Er Chieh Cho, Chi Yuan Liu, Di Wei Tang, Hsueh Yun Lee

研究成果: 雜誌貢獻 › 文章 › 同行評審

1 引文斯高帕斯（Scopus）

摘要

Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway.

原文	英語
頁（從 - 到）	1387-1401
頁數	15
期刊	Journal of Enzyme Inhibition and Medicinal Chemistry
卷	36
發行號	1
DOIs	https://doi.org/10.1080/14756366.2021.1941920
出版狀態	已發佈 - 12月 2021

ASJC Scopus subject areas

藥理
藥物發現

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10.1080/14756366.2021.1941920

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Ring size changes in the development of class I HDAC inhibitors
Lee, H. (Contributor), Cho, E. (Contributor), Tang, D. (Contributor) & Liu, C. (Contributor), figshare Academic Research System, 1月 1 2021
DOI: 10.6084/m9.figshare.14843703.v1, https://tandf.figshare.com/articles/journal_contribution/Ring_size_changes_in_the_development_of_class_I_HDAC_inhibitors/14843703/1
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title = "Ring size changes in the development of class I HDAC inhibitors",

abstract = "Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway.",

keywords = "colon cancer, HDAC, ring transformation, Thienylbenzamides",

author = "Cho, {Er Chieh} and Liu, {Chi Yuan} and Tang, {Di Wei} and Lee, {Hsueh Yun}",

note = "Funding Information: This research was supported by the Ministry of Science and Technology, Taiwan [grant no. MOST108-2320-B-038-042-MY3 and MOST 109-2320-B-038-038], Taiwan, and WanFang Hospital, Chi-Mei Medical Center, and Hualien Tzu-Chi Hospital Joint Cancer Center Grant-Focus on Colon Cancer Research [MOHW109-TDU-B-212-134020, supported by Health and welfare surcharge of tobacco products], Taiwan. Publisher Copyright: {\textcopyright} 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.",

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doi = "10.1080/14756366.2021.1941920",

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AU - Cho, Er Chieh

AU - Liu, Chi Yuan

AU - Tang, Di Wei

AU - Lee, Hsueh Yun

N1 - Funding Information: This research was supported by the Ministry of Science and Technology, Taiwan [grant no. MOST108-2320-B-038-042-MY3 and MOST 109-2320-B-038-038], Taiwan, and WanFang Hospital, Chi-Mei Medical Center, and Hualien Tzu-Chi Hospital Joint Cancer Center Grant-Focus on Colon Cancer Research [MOHW109-TDU-B-212-134020, supported by Health and welfare surcharge of tobacco products], Taiwan. Publisher Copyright: © 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.

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N2 - Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway.

AB - Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway.

KW - colon cancer

KW - HDAC

KW - ring transformation

KW - Thienylbenzamides

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Ring size changes in the development of class I HDAC inhibitors

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ASJC Scopus subject areas

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Ring size changes in the development of class I HDAC inhibitors

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