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

Authors
Gao, Y Wei, CQ Burke, TR
Citation
Y. Gao et al., Olefin metathesis in the design and synthesis of a globally constrained Grb2 SH2 domain inhibitor, ORG LETT, 3(11), 2001, pp. 1617-1620
Citations number
24
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
ORGANIC LETTERS
ISSN journal
15237060 → ACNP
Volume
3
Issue
11
Year of publication
2001
Pages
1617 - 1620
Database
ISI
SICI code
1523-7060(20010531)3:11<1617:OMITDA>2.0.ZU;2-8
Abstract
[GRAPHICS] One drawback frequently associated with olefin metathesis-mediated peptide macrocyclization, the loss of side chain functionality at sites of ring clo sure, may be circumvented by incorporation of side chain functionality with in the ring-closing olefin segments, This approach is demonstrated in the p reparation of a macrocyclic Grb2 SH2 domain antagonist designed as a confor mationally constrained beta -bend mimic.