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https://hdl.handle.net/2440/92375
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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: an international journal for chemical science, 2014; 67(9):1257-1263 |
Publisher: | CSIRO |
Issue Date: | 2014 |
ISSN: | 0004-9425 1445-0038 |
Statement of Responsibility: | 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 |
DOI: | 10.1071/CH14121 |
Grant ID: | ARC |
Published version: | http://dx.doi.org/10.1071/ch14121 |
Appears in Collections: | Aurora harvest 7 IPAS publications |
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