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

研究成果: Article同行評審

19 引文 斯高帕斯(Scopus)

摘要

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.

原文English
頁(從 - 到)141-151
頁數11
期刊European Journal of Medicinal Chemistry
131
DOIs
出版狀態Published - 2017

All Science Journal Classification (ASJC) codes

  • 藥理
  • 藥物發現
  • 有機化學

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