Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Steven G. Aitken"'
Autor:
Andrew D. Abell, Matthew A. Jones, James M. Coxon, James D. Morton, Steven G. Aitken, Stephen B. McNabb, Hannah Y.‐Y. Lee, Janna M. Mehrtens, Nathan A. Alexander, Blair G. Stuart, Axel T. Neffe, Roy Bickerstaffe
Publikováno v:
Angewandte Chemie. 121:1483-1486
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b6cad966680c7b4b07e02add87f75eb9
https://doi.org/10.1002/ange.200805014
https://doi.org/10.1002/ange.200805014
Autor:
James D. Morton, Andrew D. Abell, Roy Bickerstaffe, Blair G. Stuart, Matthew A. Jones, James M. Coxon, D. Quentin McDonald, Steven G. Aitken
Publikováno v:
Journal of medicinal chemistry. 54(21)
Studies of 17 analoges of 3 (SJA6017) in an in silico calpain model are reconciled to measured IC(50) values against ovine calpain. The studies validate the potential of the "model" and criteria established for inhibition as a tool to select structur
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9be34f4d6ea6274e16988e6be5f90ac
https://pubmed.ncbi.nlm.nih.gov/21955158
https://pubmed.ncbi.nlm.nih.gov/21955158
Autor:
Stephen B. McNabb, Steven G. Aitken, Seth A. Jones, James M. Coxon, Matthew A. Jones, Andrew D. Abell
Publikováno v:
Protein and peptide letters. 16(12)
A series of Val-Leu based peptidic aldehydes containing either a furan or thiophene at the N-terminus was prepared and assayed against ovine m-calpain. In general, potency is favoured by a 2-substituted (rather than 3-substituted) heterocycle, a thio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b01ba9fb10cb4b48b2585fe20e5a79f0
https://pubmed.ncbi.nlm.nih.gov/20001909
https://pubmed.ncbi.nlm.nih.gov/20001909
Autor:
Andrew D. Abell, Steven G. Aitken, Nathan A. Alexander, James M. Coxon, Stephen B. McNabb, Andrew C. Muscroft-Taylor, Matthew A. Jones, Hongyuan Chen
Publikováno v:
The Journal of organic chemistry. 74(11)
We report the synthesis of macrocycles 1-6 via ring closing metathesis of dienes 7-12. Addition of chlorodicyclohexylborane to thermal and microwave assisted RCM of dienes 8 and 9 markedly improves the yield. The geometric isomers of macrocycles 1-3
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::743ca87379729b7c0fb6d7f2e58a8061
https://pubmed.ncbi.nlm.nih.gov/19397301
https://pubmed.ncbi.nlm.nih.gov/19397301
Autor:
Axel T. Neffe, Blair G. Stuart, James D. Morton, Janna M. Mehrtens, James M. Coxon, Andrew D. Abell, Roy Bickerstaffe, Hannah Y.-Y. Lee, Matthew A. Jones, Steven G. Aitken, Stephen B. McNabb, Nathan A. Alexander
Publikováno v:
Angewandte Chemie (International ed. in English). 48(8)
The design and elaboration of a series of macrocyclic templates that exhibit a propensity to adopt a beta-strand-like peptide-backbone conformation led to potent and selective inhibitors of calpain 2. Macrocycle 1 retarded calcium-induced opacificati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e2ee0f1debd297feb2cc9b2dfa873f0e
https://pubmed.ncbi.nlm.nih.gov/19145612
https://pubmed.ncbi.nlm.nih.gov/19145612
Autor:
Janna M. Mehrtens, James D. Morton, Andrew D. Abell, James M. Coxon, Steven G. Aitken, Matthew A. Jones, Stephen B. McNabb, Axel T. Neffe, Roy Bickerstaffe, Shigeru Miyamoto, Hannah Y.-Y. Lee, Lucinda J. G. Robertson, Karl Gately, Jacqueline M. Wood
Publikováno v:
Bioorganicmedicinal chemistry. 16(14)
A series of N-heterocyclic dipeptide aldehydes 4-13 have been synthesised and evaluated as inhibitors of ovine calpain 1 (o-CAPN1) and ovine calpain 2 (o-CAPN2). 5-Formyl-pyrrole 9 (IC(50) values of 290 and 25nM against o-CAPN1 and o-CAPN2, respectiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa376ff734f80ecf730ba621a4b27ea2
https://pubmed.ncbi.nlm.nih.gov/18571418
https://pubmed.ncbi.nlm.nih.gov/18571418
Autor:
James M. Coxon, Stephen B. McNabb, Hannah Y.-Y. Lee, Thomas P. Cain, Axel T. Neffe, Blair G. Stuart, James D. Morton, Richard J. Payne, Andrew D. Abell, David Pearson, Matthew A. Jones, Steven G. Aitken
Publikováno v:
Journal of medicinal chemistry. 50(12)
The photoswitchable N-terminal diazo and triazene-dipeptide aldehydes 8a−d, 10a,b, and 17a,b present predominantly as the (E)-isomer, which purportedly binds deep in the S3 pocket of calpain. All compounds are potent inhibitors of m-calpain, with 8
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a70ca77e1a4f5c9335432bd6c44d4c12
https://pubmed.ncbi.nlm.nih.gov/17497840
https://pubmed.ncbi.nlm.nih.gov/17497840
Publikováno v:
ChemInform. 38
Three new classes of conformationally constrained peptidomimetics, derived from modified α- and β-amino acids, have been prepared by ring closing metathesis (RCM). The first involves Cα–N′ cyclisation of the peptidic diene (23, 24, 26), the se
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e89efdd2d87c2bd39881b5acf9e9cf95
https://doi.org/10.1002/chin.200719049
https://doi.org/10.1002/chin.200719049
Publikováno v:
Australian Journal of Chemistry. 67:1257
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 comparabl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8b05f7f46ad11b7e460e5bc513376e10
https://doi.org/10.1071/ch14121
https://doi.org/10.1071/ch14121
Autor:
Andrew D. Abell, Steven G. Aitken
Publikováno v:
Australian Journal of Chemistry. 58:3
Olefin metathesis, a process by which alkylidene groups on alkenes are exchanged, is reviewed with reference to the historical development of functional catalysts and microwave catalysis. The advent of new catalysts and improved reaction conditions h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4963fdcfb11239b3bee9b4bab0eff48a
https://doi.org/10.1071/ch04153
https://doi.org/10.1071/ch04153