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Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft.

Abstract：

:Selective estrogen receptor degraders (SERDs) have shown promise for the treatment of ER+ breast cancer. Disclosed herein is the continued optimization of our indazole series of SERDs. Exploration of ER degradation and antagonism in vitro followed by in vivo antagonism and oral exposure culminated in the discovery of indazoles 47 and 56, which induce tumor regression in a tamoxifen-resistant breast cancer xenograft.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Govek SP,Nagasawa JY,Douglas KL,Lai AG,Kahraman M,Bonnefous C,Aparicio AM,Darimont BD,Grillot KL,Joseph JD,Kaufman JA,Lee KJ,Lu N,Moon MJ,Prudente RY,Sensintaffar J,Rix PJ,Hager JH,Smith ND

doi

10.1016/j.bmcl.2015.09.074

subject

Has Abstract

pub_date

2015-11-15 00:00:00

pages

5163-7

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)30108-6

journal_volume

25

pub_type

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