含杂环残基及非经典环化RGD相关肽的合成  

Synthesis of Heterocyclic Residue Containing and Backbone Atypically Cyclized RGD Related Peptides

作　　者：韩香[1] 邱传亮[1] 龚喜[1] 杨潇骁[1] 王德心[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所,北京100050

出　　处：《化学学报》2008年第2期257-265,共9页Acta Chimica Sinica

基　　金：高等学校博士学科点专项科研基金(No．20030023037)资助项目

摘　　要：以不同的非天然结构代替RGD(Arg-Gly-Asp,精氨酰甘氨酰天冬氨酸)相关肽中的Arg残基,共合成了11个改构的RGD相关肽.其中1～8为杂环残基肽,9及10为局部杂环肽,11为丰链环肽.在合成方式上,产物1～8由传统溶液法制备,9～11经固相法制备.全部产物均由MS分析证明结构.通过本研究,为探索新型环肽合成提供了有价值的实验基础.Eleven modified RGD （Arg-Gly-Asp） peptides were synthesized by using unnatural building blocks as the surrogates for Arg residues. Three kinds of backbone structures were concerned in present products： （1） thiazolino or oxazolino residues were used instead of Arg in 1-8; （2） Arg was substituted by a locally cyclized structure between α-amino and ω-amino groups of Lys with different bridge structures in 9 and 10; （3） globally cyclized RGD analogue with ether bond bridge was used in 11. Products 1-8 were prepared by a classical solution procedure, while 9-11 were constructed on a solid support. All products were characterized by an MS analysis. It is valuable that the protocols related in present paper would afford some feasible ways to synthesize novel cyclo peptide derivatives.

关 键 词：杂环肽 非经典环化肽 RGD类似物 固相合成 杂环残基 

分 类 号：TQ464.7[化学工程—制药化工]