齐墩果酸衍生物的合成与活性，一类新型破骨细胞形成抑制剂
Synthesis and activity of oleanolic acid derivatives, a novel class of inhibitors of osteoclast formation.
作者信息
Zhang Yuan, Li Jian-xin, Zhao Jianwei, Wang Shao-zhong, Pan Yi, Tanaka Ken, Kadota Shigetoshi
机构信息
Key Lab of Analytical Chemistry for Life Science, School of Chemistry and Chemical Engineering, Nanjing University 210093, PR China.
出版信息
Bioorg Med Chem Lett. 2005 Mar 15;15(6):1629-32. doi: 10.1016/j.bmcl.2005.01.061.
Two series of oleanolic acid derivatives were synthesized and their inhibitory activity on the formation of osteoclast-like multinucleated cells (OCLs) induced by 1alpha,25-dihydroxy vitamin D3 was evaluated in a co-culture assay system. The structure-activity relationships, together with electronic structure based on the frontier molecular orbitals, for example, HOMO and LUMO, related to different amino acid substituents were studied. Derivatives with proline or phenylalanine showed a tendency to enhance the inhibitory activity.
合成了两系列齐墩果酸衍生物，并在共培养测定系统中评估了它们对1α,25 - 二羟基维生素D3诱导的破骨细胞样多核细胞（OCLs）形成的抑制活性。研究了与不同氨基酸取代基相关的结构 - 活性关系，以及基于前沿分子轨道（例如HOMO和LUMO）的电子结构。含有脯氨酸或苯丙氨酸的衍生物显示出增强抑制活性的趋势。
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