发现新型苯并[b][1,4]恶嗪-3(4H)-酮类化合物作为聚（ADP-核糖）聚合酶抑制剂。
Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors.
机构信息
Takeda California, 10410 Science Center Dr, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2013 Aug 15;23(16):4501-5. doi: 10.1016/j.bmcl.2013.06.055. Epub 2013 Jun 24.
PMID:23850199
Abstract
Structure based drug design of a series of novel 1,4-benzoxazin-3-one derived PARP-1 inhibitors are described. The synthesis, enzymatic & cellular activities and pharmacodynamic effects are described. Optimized analogs demonstrated inhibition of poly-ADP-ribosylation in SW620 tumor bearing nude mice through 24h following a single dose.
摘要
描述了一系列新型 1,4-苯并恶嗪-3-酮衍生的 PARP-1 抑制剂的基于结构的药物设计。描述了它们的合成、酶学和细胞活性以及药效学作用。优化后的类似物在单次给药后 24 小时内通过 SW620 荷瘤裸鼠证明了多聚 ADP-核糖基化的抑制作用。
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