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

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Hsieh MT,Chang LC,Hung HY,Lin HY,Shih MH,Tsai CH,Kuo SC,Lee KH

doi

10.1016/j.ejmech.2017.03.006

subject

Has Abstract

pub_date

2017-05-05 00:00:00

pages

141-151

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)30155-1

journal_volume

131

pub_type

杂志文章

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