SAR Based Design of Nicotinamides as a Novel Class of Androgen Receptor Antagonists for Prostate Cancer

详细信息    查看全文

• 作者：Su Hui Yang ; Chin-Hee Song ; Hue Thi My Van ; Eunsook Park ; Daulat Bikram Khadka ; Eun-Yeung Gong ; Keesook Lee ; Won-Jea Cho
• 刊名：Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：April 25, 2013
• 年：2013
• 卷：56
• 期：8
• 页码：3414-3418
• 全文大小：369K
• 年卷期：v.56,no.8(April 25, 2013)
• ISSN：1520-4804

文摘

Molecular knowledge of pure antagonism and systematic SAR study offered a direction for structural optimization of DIMN to provide nicotinamides as a novel series of AR antagonists. Nicotinamides with extended linear scaffold bearing sterically bulky alkoxy groups on isoquinoline end were synthesized for H12 displacement. AR binding affinity and molecular basis of antiandrogenic effect establish the optimized derivatives, 7au and 7bb, as promising candidates of second generation AR antagonists for advanced prostate cancer.