Substituted piperidines as HDM2 inhibitors

详细信息    查看全文

• 作者：Yao Ma ; Brian R. Lahue ; Gerald W. Shipps Jr. ; Jeseca Brookes ; Yaolin Wang
• 关键词：HDM2 ; MDM2 ; p53 ; Substituted piperidine ; Small molecule inhibitor ; Cancer ; Oncology
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 February, 2014
• 年：2014
• 卷：24
• 期：4
• 页码：1026-1030
• 全文大小：4818 K

文摘

Novel small molecule HDM2 inhibitor, substituted piperidine, was identified. Initial SAR study indicated potential for several position optimizations. Additional potency enhancement was achieved by introducing a sidechain off the aromatic ring. DMPK study of one of the active compounds has shown a moderate oral PK and reasonable bioavailability.