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OALib Journal期刊
ISSN: 2333-9721
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氮杂吲哚类parp-1抑制剂的合成及活性评价
, PP. 1792-1799
Keywords: parp-1,抑制剂,氮杂吲哚,抗肿瘤药物
Abstract:
parp-1通过催化adp-核糖单元（adp-ribose）从烟酰胺腺嘌呤二核苷酸（nicotinamideadeninedinucleotide，nad+）转移至各种底物蛋白上，参与损伤dna的修复过程，是潜在的新机制的抗肿瘤药物靶标。本文设计合成了新结构氮杂吲哚类目标化合物16个，获得了对parp-1具有抑制活性的化合物8个，其中2-位为脂环胺取代的氮杂吲哚对parp-1和parp-2均有抑制活性。
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