New bis(hydroxymethyl) alkanoate curcuminoid derivatives exhibit activity against triple-negative breast cancer in vitro and in vivo

Min Tsang Hsieh, Ling Chu Chang, Hsin Yi Hung, Hui Yi Lin, Mei Hui Shih, Chang Hai Tsai, Sheng Chu Kuo, Kuo Hsiung Lee

Research output: Contribution to journalArticle

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Abstract

Novel bis(hydroxymethyl) alkanoate curcuminoid derivatives were designed, synthesized and screened for in vitro antiproliferative and in vivo antitumor activity. Selected new compound 9a and curcumin were further evaluated for inhibitory activity against ER+/PR+ breast cancer (MCF-7, T47D), HER 2+ breast cancer (SKBR3, BT474, and MDA-MB-457) and triple negative breast cancer (TNBC) (HS-578T, MDA-MB-157, and MDA-MB-468) cell lines. In addition, compound 9a was evaluated in the MDA-MB-231 xenograft nude mice model. Compound 9a exhibited greater inhibitory activity than curcumin against TNBC cells and also demonstrated significant inhibitory activity against doxorubicin-resistant MDA-MB-231 cells, with ten-fold higher potency than curcumin. Furthermore, when evaluated against the MDA-MB-231 xenograft nude mice model, compound 9a alone was ten-fold more potent than curcumin. Moreover, synergistic activity was observed when 9a was used in combination with doxorubicin against MDA-MB-231 breast cancer cells.

LanguageEnglish (US)
Pages141-151
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume131
DOIs
StatePublished - May 5 2017

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Triple Negative Breast Neoplasms
Curcumin
Derivatives
Breast Neoplasms
Heterografts
Nude Mice
Doxorubicin
Cells
Cell Line
In Vitro Techniques

Keywords

  • Antiproliferative agents
  • Antitumor agents
  • Bis(hydroxymethyl) alkanoate curcuminoids
  • Curcumin
  • Triple-negative breast cancer

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Cite this

New bis(hydroxymethyl) alkanoate curcuminoid derivatives exhibit activity against triple-negative breast cancer in vitro and in vivo. / Hsieh, Min Tsang; Chang, Ling Chu; Hung, Hsin Yi; Lin, Hui Yi; Shih, Mei Hui; Tsai, Chang Hai; Kuo, Sheng Chu; Lee, Kuo Hsiung.

In: European Journal of Medicinal Chemistry, Vol. 131, 05.05.2017, p. 141-151.

Research output: Contribution to journalArticle

Hsieh, Min Tsang ; Chang, Ling Chu ; Hung, Hsin Yi ; Lin, Hui Yi ; Shih, Mei Hui ; Tsai, Chang Hai ; Kuo, Sheng Chu ; Lee, Kuo Hsiung. / New bis(hydroxymethyl) alkanoate curcuminoid derivatives exhibit activity against triple-negative breast cancer in vitro and in vivo. In: European Journal of Medicinal Chemistry. 2017 ; Vol. 131. pp. 141-151
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