Health & Environmental Research Online (HERO)


Print Feedback Export to File
6323150 
Journal Article 
Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft 
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 
2015 
Yes 
Bioorganic & Medicinal Chemistry Letters
ISSN: 0960-894X
EISSN: 1464-3405 
25 
22 
5163-5167 
English 
26463130 
WOS:000364535000028 
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.