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中文摘要：
CD38是一种多功能的跨膜糖蛋白,其酶催化活性与哺乳动物体内多种疾病的发生和发展密切相关。本文以CD38抑制剂H2为先导结构,将其吲哚母环替换为嘌呤环,设计合成了33个嘌呤衍生物,活性评价结果显示化合物20、38表现出与先导结构相当的抗CD38 NADase活性。研究结果揭示嘌呤6位小取代基对化合物活性的影响不大,嘌呤2-位是否有苯丙酰基取代对化合物与CD38的结合模式有重要影响。
英文摘要：
CD38 is a multifunctional enzyme expressed in a variety of mammalian tissues, its catalytic activity was involved in a wide range of physiological processes. Based on the reported inhibitor of human CD38 NADase, 33 purine derivatives were designed and synthesized. The biological activity assay showed that compounds 20 and 38 exhibited almost the same extent of inhibitory activities on human CD38 NADase as the lead compound H2. The results also revealed that small substituents at C-6 of purine ring gave no obvious effect on inhibitory activity, but phenylpropionyl moiety at N-2 could affect the binding mode of the compound with CD38. This study provides a reliable basis for future rational design of inhibitors for CD38.
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