β-Alkylthio indolyl carbinols: Potent nonsteroidal antiandrogens with oral efficacy in a prostate cancer model

Through an in vivo screening model, we developed the in vivo SAR of β-alkylthio indolyl carbinols. Through these efforts we identified a compound with potent oral in vivo efficacy in both immature and mature rat prostate weight reduction models and in a murine xenograft prostate cancer model.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-05, Vol.17 (9), p.2545-2548
Hauptverfasser:	Lanter, James C., Fiordeliso, James J., Alford, Vernon C., Zhang, Xuqing, Wells, Kenneth M., Russell, Ronald K., Allan, George F., Lai, Muh-Tsann, Linton, Olivia, Lundeen, Scott, Sui, Zhihua
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Androgen Antagonists - chemical synthesis Androgen Antagonists - pharmacology Androgen receptor Animals Antineoplastic agents Antineoplastic Agents - administration & dosage Antineoplastic Agents - chemical synthesis Bioisostere Biological and medical sciences Chemistry, Pharmaceutical - methods Disease Models, Animal Drug Design Drug Screening Assays, Antitumor General aspects Indoles - chemical synthesis Indoles - pharmacology Male Medical sciences Methanol - analogs & derivatives Methanol - chemistry Mice Neoplasm Transplantation Pharmacology. Drug treatments Prostatic Neoplasms - drug therapy Rats Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	Through an in vivo screening model, we developed the in vivo SAR of β-alkylthio indolyl carbinols. Through these efforts we identified a compound with potent oral in vivo efficacy in both immature and mature rat prostate weight reduction models and in a murine xenograft prostate cancer model.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.02.014