| Title of Article |
Influence of side-chain changes on histone deacetylase inhibitory and
cytotoxicity activities of curcuminoid derivatives |
| Date of Acceptance |
5 April 2020 |
| Journal |
| Title of Journal |
ิิิBioorganic & Medicinal Chemistry Letters |
| Standard |
SCOPUS |
| Institute of Journal |
© 2020 Elsevier B.V. |
| ISBN/ISSN |
0960-894y |
| Volume |
2020 |
| Issue |
11 |
| Month |
June |
| Year of Publication |
2020 |
| Page |
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 g/mL and 7.33 ± 0.98 g/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. |
| Keyword |
Curcumin, Histonedeacetylase, anticancer |
| Author |
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| Reviewing Status |
มีผู้ประเมินอิสระ |
| Status |
ตีพิมพ์แล้ว |
| Level of Publication |
นานาชาติ |
| citation |
true |
| Part of thesis |
true |
| Attach file |
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| Citation |
0
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Publication
Journal Publication
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