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

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 22, 2015, Pages 5163-5167

  Govek, Steven P ^a   Nagasawa, Johnny Y ^a   Douglas, Karensa L ^a   Lai, Andiliy G ^a   Kahraman, Mehmet ^a   Bonnefous, Celine ^a   Aparicio, Anna M ^a   Darimont, Beatrice D ^a   Grillot, Katherine L ^a   Joseph, James D ^a   Kaufman, Joshua A ^a   Lee, Kyoung Jin ^a   Lu, Nhin ^a   Moon, Michael J ^a   Prudente, Rene Y ^a   Sensintaffar, John ^a   Rix, Peter J ^a   Hager, Jeffrey H ^a   Smith, Nicholas D ^a  

^a Seragon Pharmaceuticals   (United States)

Author keywords

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

Indexed keywords

ANTINEOPLASTIC AGENT; ANTINEOPLASTIC HORMONE AGONISTS AND ANTAGONISTS; ARN 810; ESTROGEN RECEPTOR ANTAGONIST; FULVESTRANT; INDAZOLE DERIVATIVE; TAMOXIFEN; UNCLASSIFIED DRUG; 3-(4-(2-(2-CHLORO-4-FLUOROPHENYL)-1-(1H-INDAZOL-5-YL)BUT-1-EN-1-YL)PHENYL)ACRYLIC ACID; CINNAMIC ACID DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CANCER; CANCER REGRESSION; CANCER RESISTANCE; CELL VIABILITY; CONTROLLED STUDY; FEMALE; IC50; IN VITRO STUDY; IN VIVO STUDY; LIPOPHILICITY; MOUSE; NONHUMAN; PROCESS OPTIMIZATION; RAT; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT; ANIMAL; BREAST NEOPLASMS; CHEMISTRY; DRUG RESISTANCE; DRUG SCREENING; METABOLISM; PATHOLOGY;

ANIMALS; ANTINEOPLASTIC AGENTS; BREAST NEOPLASMS; CINNAMATES; DRUG RESISTANCE, NEOPLASM; ESTROGEN RECEPTOR ANTAGONISTS; FEMALE; INDAZOLES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TAMOXIFEN; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84945967308     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.09.074     Document Type: Article

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