发现和 SAR 新型、强效和选择性六氢苯并萘啶酮抑制剂聚（ADP-核糖）聚合酶-1（PARP-1）。
Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
机构信息
IRBM-Merck Research Laboratories Rome, Via Pontina km 30,600, Pomezia, 00040 Rome, Italy.
出版信息
Bioorg Med Chem Lett. 2010 Jan 15;20(2):448-52. doi: 10.1016/j.bmcl.2009.12.002. Epub 2009 Dec 4.
PMID:20015648
Abstract
A novel hexahydrobenzonaphthyridinone PARP-1 pharmacophore is reported, subsequent SAR exploration around this scaffold led to selective PARP-1 inhibitors with low nanomolar enzyme potency, displaying good cellular activity and promising rat PK properties.
摘要
报道了一种新型六氢苯并萘啶酮 PARP-1 药效团，随后围绕该骨架进行了 SAR 探索，得到了具有低纳摩尔酶活性的选择性 PARP-1 抑制剂，具有良好的细胞活性和有前景的大鼠 PK 性质。
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