2. Academic Validation
  3. Influence of side-chain changes on histone deacetylase inhibitory and cytotoxicity activities of curcuminoid derivatives

Influence of side-chain changes on histone deacetylase inhibitory and cytotoxicity activities of curcuminoid derivatives

  • Bioorg Med Chem Lett. 2020 Jun 1;30(11):127171. doi: 10.1016/j.bmcl.2020.127171.
La-Or Somsakeesit 1,  Thanaset Senawong 2,  Pakit Kumboonma 3,  Somprasong Saenglee 4,  Arunta Samankul 2,  Gulsiri Senawong 2,  Chavi Yenjai 1,  Chanokbhorn Phaosiri 5
Affiliations

Affiliations

  • 1 Natural Products Research Unit, Center of Excellence for Innovation in Chemistry, Ministry of Higher Education, Science, Research and Innovation (Implementation Unit-IU, Khon Kaen University), Department of Chemistry, Faculty of Science, Khon Kaen University, Khon Kaen 40002, Thailand.
  • 2 Natural Products Research Unit, Department of Biochemistry, Faculty of Science, Khon Kaen University, Khon Kaen 40002, Thailand.
  • 3 Department of Applied Chemistry, Faculty of Science and Liberal Arts, Rajamangala University of Technology Isan, Nakhon Ratchasima 30000, Thailand.
  • 4 Ban Dong Subdistrict Administration Organization, Ubolratana District, Khon Kaen 40250, Thailand.
  • 5 Natural Products Research Unit, Center of Excellence for Innovation in Chemistry, Ministry of Higher Education, Science, Research and Innovation (Implementation Unit-IU, Khon Kaen University), Department of Chemistry, Faculty of Science, Khon Kaen University, Khon Kaen 40002, Thailand. Electronic address: chapha@kku.ac.th.
PMID: 32273215 DOI: 10.1016/j.bmcl.2020.127171
Abstract

Using curcuminoids as lead compounds, fifty-nine curcuminoid derivatives with different side chains at the phenolic moiety were synthesized. All compounds were investigated for their histone deacetylase (HDAC) inhibitory activities. The potent pan-HDAC inhibitors were further tested against three human Cancer cell lines including Hela, HCT116 and MCF-7 with MTT-based assay. The bisethylamide 4z and the mono-sec-butyl derivative 5j manifested good antiproliferative activities against HCT116 Cancer cells with the IC50 values as 14.60 ± 1.19 μg/mL and 7.33 ± 0.98 μg/mL, respectively. Molecular docking study of both compounds with Class I HDACs revealed that the compounds might bind tightly to the binding pocket of HDAC2. These findings suggested that these compounds can be putative candidates for the development of Anticancer drugs via inhibiting HDACs.

Keywords

Anticancer; Curcumin; HDAC; Turmeric.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z