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

1 Citation (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)

Access to Document

10.1080/14756366.2021.1941920

Cite this

@article{dfa5f093e63741c2a0b3d863840e295d,

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.",

year = "2021",

month = dec,

doi = "10.1080/14756366.2021.1941920",

language = "English",

volume = "36",

pages = "1387--1401",

journal = "Journal of Enzyme Inhibition and Medicinal Chemistry",

issn = "1475-6366",

publisher = "Informa Healthcare",

number = "1",

}

TY - JOUR

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

UR - http://www.scopus.com/inward/record.url?scp=85108951819&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85108951819&partnerID=8YFLogxK

U2 - 10.1080/14756366.2021.1941920

DO - 10.1080/14756366.2021.1941920

M3 - Article

C2 - 34167419

AN - SCOPUS:85108951819

SN - 1475-6366

VL - 36

SP - 1387

EP - 1401

JO - Journal of Enzyme Inhibition and Medicinal Chemistry

JF - Journal of Enzyme Inhibition and Medicinal Chemistry

IS - 1

ER -

Ring size changes in the development of class I HDAC inhibitors

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

Other files and links

Fingerprint