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Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft.
Govek, Steven P; Nagasawa, Johnny Y; Douglas, Karensa L; Lai, Andiliy G; Kahraman, Mehmet; Bonnefous, Celine; Aparicio, Anna M; Darimont, Beatrice D; Grillot, Katherine L; Joseph, James D; Kaufman, Joshua A; Lee, Kyoung-Jin; Lu, Nhin; Moon, Michael J; Prudente, Rene Y; Sensintaffar, John; Rix, Peter J; Hager, Jeffrey H; Smith, Nicholas D.
Affiliation
  • Govek SP; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States. Electronic address: sgovek@seragonpharm.com.
  • Nagasawa JY; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Douglas KL; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Lai AG; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Kahraman M; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Bonnefous C; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Aparicio AM; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Darimont BD; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Grillot KL; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Joseph JD; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Kaufman JA; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Lee KJ; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Lu N; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Moon MJ; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Prudente RY; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Sensintaffar J; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Rix PJ; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Hager JH; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
  • Smith ND; Seragon Pharmaceuticals, Inc., 12780 El Camino Real, Suite 302, San Diego, CA 92130, United States.
Bioorg Med Chem Lett ; 25(22): 5163-7, 2015 Nov 15.
Article in En | MEDLINE | ID: mdl-26463130
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Tamoxifen / Breast Neoplasms / Estrogen Receptor Antagonists / Indazoles / Antineoplastic Agents Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2015 Document type: Article
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Tamoxifen / Breast Neoplasms / Estrogen Receptor Antagonists / Indazoles / Antineoplastic Agents Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2015 Document type: Article