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Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.

Abstract：

:HER2 overexpression is associated with aggressive breast cancer with high recurrence rate and poor patient prognosis. Treatment of HER2 overexpressing patients with the HER2 targeting therapy trastuzumab results in acquired resistance within a year. The HER2/EGFR dual kinase inhibitor lapatinib was shown to inhibit some trastuzumab resistant breast cancer cell lines and is currently in clinical trials. Our group has found two new quinone compounds that show excellent inhibition of breast tumor cells expressing HER2 or the trastuzumab resistant HER2 oncogenic isoform, HER2Δ16. Compound 4 ((1R,2S,3S)-1,2,3,5,8-pentahydroxy-1,2,3,4-tetrahydroanthracene-9,10-dione) and compound 5 (5,8-dihydroxy-2,3-bis(hydroxymethyl)naphthalene-1,4-dione) showed sub-micromolar inhibition potency against these cell lines. These compounds also inhibit auto-phosphorylation of the Y1248 and Y1068 residues of HER2 and EGFR, respectively.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Sridhar J,Sfondouris ME,Bratton MR,Nguyen TL,Townley I,Klein Stevens CL,Jones FE

doi

10.1016/j.bmcl.2013.11.064

subject

Has Abstract

pub_date

2014-01-01 00:00:00

pages

126-31

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)01355-3

journal_volume

24

pub_type

杂志文章

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