2. Academic Validation
  3. Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft

Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft

  • Bioorg Med Chem Lett. 2019 Feb 1;29(3):367-372. doi: 10.1016/j.bmcl.2018.12.042.
Steven P Govek 1,  Celine Bonnefous 2,  Jackaline D Julien 2,  Johnny Y Nagasawa 2,  Mehmet Kahraman 2,  Andiliy G Lai 2,  Karensa L Douglas 2,  Anna M Aparicio 2,  Beatrice D Darimont 2,  Katherine L Grillot 2,  James D Joseph 2,  Joshua A Kaufman 2,  Kyoung-Jin Lee 2,  Nhin Lu 2,  Michael J Moon 2,  Rene Y Prudente 2,  John Sensintaffar 2,  Peter J Rix 2,  Jeffrey H Hager 2,  Nicholas D Smith 2
Affiliations

Affiliations

  • 1 Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States. Electronic address: sgovek@san.rr.com.
  • 2 Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
PMID: 30587451 DOI: 10.1016/j.bmcl.2018.12.042
Abstract

Potent Estrogen Receptor ligands typically contain a phenolic hydrogen-bond donor. The indazole of the selective Estrogen receptor Degrader (SERD) ARN-810 is believed to mimic this. Disclosed herein is the discovery of ARN-810 analogs which lack this hydrogen-bond donor. These SERDs induced tumor regression in a tamoxifen-resistant breast Cancer xenograft, demonstrating that the indazole NH is not necessary for robust ER-modulation and anti-tumor activity.

Keywords

Breast cancer; Degrader; Estrogen receptor; SERD; Tamoxifen-resistant.

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