Synthesis and biological evaluation of immunosuppressive agent DZ2002 and its stereoisomers

摘要：

DZ2002 and its related stereoisomers were efficiently synthesized. The optical data of (R)and (S)-DZ2002 were disclosed here for the first time. Their inhibitory potency was evaluated on SAHase and MLR assay in the mean time. In accordance with respective inhibitory potency of SAHase, the immuno-suppressive potency order was demonstrated as (S)-DZ2002>(Rac)-DZ2002>(R)-DZ2002>(Keto)-DZ2002. These results indicate (S)-configuration of 2-chiral center in DZ2002 is important for binding with SAHase.

关键词： DZ2002 Stereoisomers Synthesis Immunosuppressive potency S-Adenosyl-L-homocysteine hydrolase

作者: Yang-Ming Zhang Yu Ding Wei Tang Wei Luo Min Gu Wei Lu Jie Tang Jian-Ping Zuo Fa-Jun Nan

作者单位: Department of Chemistry and Institute of Medicinal Chemistry, East China Normal University, 3663 Nor Department of Immunopharmacology.State Key Laboratory of Drug Research, Shanghai Institute of Materi The National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Department of Chemistry and Institute of Medicinal Chemistry, East China Normal University, 3663 Nor

会议类型: 国际会议

会议名称: 第四届国际分子模拟与信息技术应用学术会议(The 4th International Conference of Molecular Simulations and Applied Informatics Technologies)

会议地点: 广州

会议语种:英文

页码: 458-462

在线出版日期: 2008-11-01（万方平台首次上网日期，不代表论文的发表时间）