Olefin metathesis in the design and synthesis of a globally constrained Grb2 SH2 domain inhibitor |
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Authors: | Gao Y Wei C Q Burke T R |
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Institution: | Laboratory of Medicinal Chemistry, DBS, NCI-FCRDC, National Institutes of Health, Frederick, MD 20892-4255, USA. |
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Abstract: | 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. |
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