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

Research output: Contribution to journal › Article › peer-review

3 Citations (Scopus)

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.

Original language	English
Pages (from-to)	1387-1401
Number of pages	15
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Volume	36
Issue number	1
DOIs	https://doi.org/10.1080/14756366.2021.1941920
Publication status	Published - Dec 2021

Keywords

colon cancer
HDAC
ring transformation
Thienylbenzamides

ASJC Scopus subject areas

Pharmacology
Drug Discovery

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1080/14756366.2021.1941920

Cite this

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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}",

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year = "2021",

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doi = "10.1080/14756366.2021.1941920",

language = "English",

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T1 - Ring size changes in the development of class I HDAC inhibitors

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.

PY - 2021/12

Y1 - 2021/12

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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JO - Journal of Enzyme Inhibition and Medicinal Chemistry

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ER -

Ring size changes in the development of class I HDAC inhibitors

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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