The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening

Autor:	Muh-Tsann Lai, Weiqin Jiang, Zhihua Sui, James C. Lanter, Do Won Hahn, George F. Allan, Olivia Linton, James J. Fiordeliso, Scott G. Lundeen
Rok vydání:	2007
Předmět:	Male Indoles medicine.drug_class Clinical Biochemistry Drug Evaluation Preclinical Administration Oral Pharmaceutical Science Pharmacology Antiandrogen Biochemistry Tosyl Compounds Structure-Activity Relationship chemistry.chemical_compound In vivo Nitriles Drug Discovery Androgen Receptor Antagonists medicine Animals Structure–activity relationship Potency Anilides Molecular Biology Indole test Chemistry Organic Chemistry Prostate Androgen Antagonists Rats Androgen receptor Molecular Medicine Bioisostere
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 17:123-126
ISSN:	0960-894X
Popis:	A series of novel 2-(1H-indol-2-yl)-propan-2-ols have been designed, synthesized, and screened for their ability to inhibit testosterone-induced prostate weight increases in immature rats. Through the use of this paradigm, we were able to identify compounds that exhibited in vivo potency equal to that of the marketed antiandrogen Casodex when orally administered.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::041cce7063cd70cb352a308467308f11 https://doi.org/10.1016/j.bmcl.2006.09.086 Zobrazit plný text záznamu Full Text from ScienceDirect