| Literature DB >> 26463130 |
Steven P Govek1, Johnny Y Nagasawa2, Karensa L Douglas2, Andiliy G Lai2, Mehmet Kahraman2, Celine Bonnefous2, Anna M Aparicio2, Beatrice D Darimont2, Katherine L Grillot2, James D Joseph2, Joshua A Kaufman2, Kyoung-Jin Lee2, Nhin Lu2, Michael J Moon2, Rene Y Prudente2, John Sensintaffar2, Peter J Rix2, Jeffrey H Hager2, Nicholas D Smith2.
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.Entities:
Keywords: Breast cancer; Degrader; Estrogen receptor; SERD; Tamoxifen-resistant
Mesh：
Substances：
Year: 2015 PMID： 26463130 DOI： 10.1016/j.bmcl.2015.09.074
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823