title: [The synthesis of purine derivatives and its inhibitory activity on CD38 NADase].
abstract: 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.
authors.forename: Na
authors.initials: N
authors.lastname: Li
authors.forename: Wen-jie
authors.initials: WJ
authors.lastname: Zhu
authors.forename: Xi-wen
authors.initials: XW
authors.lastname: Xue
authors.forename: Yong-juan
authors.initials: YJ
authors.lastname: Zhao
authors.forename: Hon-cheung
authors.initials: HC
authors.lastname: Lee
authors.forename: Liang-ren
authors.initials: LR
authors.lastname: Zhang
authors.forename: Li-he
authors.initials: LH
authors.lastname: Zhang
mesh_terms: D051997:ADP-ribosyl Cyclase 1 / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D011687:Purines / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D004791:Enzyme Inhibitors; D011687:Purines; D051997:ADP-ribosyl Cyclase 1