Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase
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- 作者：Keith A. Menear ; Claire Adcock ; Francisco Cuenca Alonso ; Kristel Blackburn ; Louise Copsey ; Jan Drzewiecki ; Alex ; ra Fundo ; Armelle Le Gall ; Sylvie Gomez ; Hashim Javaid ; Carlos Fen ; ez Lence ; Niall M.B.
- 关键词：Poly(ADP-ribose) polymerase-1 ; PARP-1 ; PARP-2
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：15 July 2008
- 年：2008
- 卷：18
- 期：14
- 页码：3942-3945
- 全文大小：172 K
文摘
We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed with restricted conformation through intramolecular hydrogen bond formation; the compounds exhibit low nM enzyme and cellular activity as PARP-1 inhibitors.