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Identification of 5-nitrofuran-2-amide derivatives that induce apoptosis in triple negative breast cancer cells by activating C/EBP-homologous protein expression.

Abstract：

:The transcription factor C/EBP-homologous protein (CHOP) is a key component of the terminal unfolded protein response (UPR) that mediates unresolvable endoplasmic reticulum stress-induced apoptosis. CHOP induction is known to cause cancer cell death. Chemicals that induce CHOP expression would thus be valuable as potential cancer therapeutics and as research tools. Here, we identified 5-nitrofuran-2-amide derivatives as small molecule activators of CHOP expression that induced apoptosis in triple negative breast cancer (TNBC) cells. Our preliminary structure-activity relationship studies indicated that compounds with an N-phenyl-5-nitrofuran-2-carboxamide skeleton were particularly potent inducers of TNBC cell apoptosis. The compounds activate CHOP expression via the PERK-eIF2α-ATF4 branch of the UPR. These results indicate that small molecule activators of CHOP expression may have therapeutic potential for TNBC.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Duan H,Li Y,Lim HY,Wang W

doi

10.1016/j.bmc.2015.06.011

subject

Has Abstract

pub_date

2015-08-01 00:00:00

pages

4514-4521

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(15)00505-2

journal_volume

23

pub_type

杂志文章

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