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J Enzyme Inhib Med Chem
J Enzyme Inhib Med Chem
Journal of Enzyme Inhibition and Medicinal Chemistry
1475-6366
1475-6374
Taylor & Francis

10.1080/14756366.2021.1941920
1941920
Version of Record
Research Article
Research Paper
Ring size changes in the development of class I HDAC inhibitors
E.-C. Cho et al.
Cho Er-Chieh abc
Liu Chi-Yuan a
Tang Di-Wei a
Lee Hsueh-Yun ad
a School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan
b Master Program in Clinical Genomics and Proteomics, College of Pharmacy, Taipei Medical University, Taipei, Taiwan
c Cancer Center, Wan Fang Hospital, Taipei Medical University, Taipei, Taiwan
d Ph.D. Program in Drug Discovery and Development Industry, College of Pharmacy, Taipei Medical University, Taipei, Taiwan
# Contributed equally to this work.

Supplemental data for this article can be accessed here.

CONTACT Hsueh-Yun Lee kmontoya@example.org of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan; Ph.D. Program in Drug Discovery and Development Industry, College of Pharmacy, Taipei Medical University, Taipei, Taiwan
24 6 2021
2021
36 1 13871401
Supplemental Material

Click here for additional data file.

© 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.
2021
The Author(s)
https://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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.

Graphical Abstract

Keywords

Thienylbenzamides
ring transformation
HDAC
colon cancer
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.


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