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Type: Journal article
Title: The preparation of macrocyclic calpain inhibitors by ring closing metathesis and cross metathesis
Author: Jones, S.
Duncan, J.
Aitken, S.
Coxon, J.
Abell, A.
Citation: Australian Journal of Chemistry, 2014; 67(9):1257-1263
Publisher: CSIRO
Issue Date: 2014
ISSN: 0004-9425
Statement of
Seth A. Jones, Joanna Duncan, Steven G. Aitken, James M. Coxon and Andrew D. Abell
Abstract: Ring closing metathesis and cross metathesis approaches to a new macrocyclic peptidomimetic aldehyde 2 have been developed, with the former route being the most convenient. Aldehyde 2 is a potent inhibitor of calpain II (IC50 of 45 nM) with comparable activity to the benchmark acyclic inhibitor SJA6017 4. Both compounds contain an N-terminal 4-fluorophenylsulfonyl group. The P2 Ile analogue of 2 (16) is significantly less active (IC50 of 2000 nM) which reflects an unusually subtle importance of the P2 residue for active site binding.
Rights: Copyright status unknown
RMID: 0030010017
DOI: 10.1071/CH14121
Appears in Collections:IPAS publications

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