Olefin metathesis in the design and synthesis of a globally constrained Grb2 SH2 domain inhibitor

被引：43

作者：

Gao, Y ^{[1
]}

Wei, CQ ^{[1
]}

Burke, TR ^{[1
]}

机构：

[1] NCI, Med Chem Lab, DBS, FCRDC,NIH, Frederick, MD 20892 USA

来源：

ORGANIC LETTERS | 2001年 / 3卷 / 11期

关键词：

D O I：

10.1021/ol0157609

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] One drawback frequently associated with olefin metathesis-mediated peptide macrocyclization, the loss of side chain functionality at sites of ring closure, may be circumvented by incorporation of side chain functionality within the ring-closing olefin segments, This approach is demonstrated in the preparation of a macrocyclic Grb2 SH2 domain antagonist designed as a conformationally constrained beta -bend mimic.

引用

页码：1617 / 1620

页数：4

共 24 条

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