NOUVEAUX ANTIANDROGENES/INHIBITEURS DE CYP17 C-17-HETEROARYLE STEROIDES: SYNTHESE, ACTIVITES BIOLOGIQUES IN VITRO, PHARMACOCINETIQUE ET ACTIVITE ANTITUMORALE

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专利权人:

UNIVERSITY OF MARYLAND; BALTIMORE

发明人:

BRODIE, ANGELA,NJAR, VINCENT

申请号：

CA2599953

公开号：

CA2599953C

申请日:

2006.03.02

申请国别(地区):

CA

年份:

2013

代理人:

摘要：

Described are steroidal C- 17 benzoazoles, pyrimidinoazoles (azabenzoazoles)and diazines. Methods for their synthesis are also described, which includemethods having a step of nucleophilic vinylic "addition-elimination"substitution reaction of 3.beta.-acetoxy-17- chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles andmethods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3.beta.-ol or analogs thereof with tributylstannyldiazines. The compounds are potent inhibitors of human CYP 17 enzyme as wellas potent antagonists of both wild type and mutant androgen receptors (AR).The compounds are useful for the treatment of human prostate cancer.

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