Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Sandra Moreno-Mazza"'
Autor:
Ingrid Mechin, Chris Arendt, Mikhail Levit, Claude Barberis, Sandra Moreno-Mazza, Tahir Majid, Neil Moorcroft, Joseph D. Batchelor
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:4730-4734
Novel N-substituted azaindoles have been discovered as PIM1 inhibitors. X-ray structures have played a significant role in orienting the chemistry effort in the initial phase of hit confirmation. Disclosure of an unconventional binding mode for 1 and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c6e345aa610ffd7e7fdccac9ab3f3502
https://doi.org/10.1016/j.bmcl.2017.08.069
https://doi.org/10.1016/j.bmcl.2017.08.069
Autor:
James Pribish, Claude Barberis, Liduo Shen, Mark Czekaj, Neil Moorcroft, Mikhail Levit, Elina Tserlin, Anlai Wang, Andrew Hebert, Sandra Moreno-Mazza, Matthieu Barrague, Tahir Majid, Joseph D. Batchelor, Paul Erdman, Alexandre Gross
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(20)
N-Substituted azaindoles have been discovered as pan-PIM kinase inhibitors. Initial SAR, early ADME and PK/PD data of a series of compounds is described and led to the identification of promising pan-PIM inhibitors which validated our interest in the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5e12991c47405661b7be0ce261b38b7
https://pubmed.ncbi.nlm.nih.gov/28927793
https://pubmed.ncbi.nlm.nih.gov/28927793
Autor:
Stuart Emanuel, Lee M. Greenberger, Guozhang Xu, Sandra Moreno-Mazza, Niranjan Pandey, Steven A. Middleton, Peter J. Connolly, Prabha Karnachi, Steven K. Wetter, Terry V. Hughes, Mary Adams, Scott R. Pollack
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4896-4899
A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine was synthesized and found to have potent dual EGFR/HER2 kinase inhibitory activity. The structure-based drug design of this molecule as well as the kinase and cellular inhibition of HER2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03fc06459e8de9b189b2ea8e7ec097ab
https://doi.org/10.1016/j.bmcl.2008.07.057
https://doi.org/10.1016/j.bmcl.2008.07.057
Autor:
Sandra Moreno-Mazza, Stuart Emanuel, Peter J. Connolly, Niranjan Pandey, Robert H. Gruninger, Lee M. Greenberger, Virna Borowski, Steven A. Middleton, Terry V. Hughes, Jennifer R. Story, Cheryl Napier, Jeannene Butler, Mary Adams, Beth A. Hollister, Catherine A. Rugg, Angel R. Fuentes‐Pesquera
Publikováno v:
Molecular Pharmacology. 73:338-348
JNJ-28871063 is a potent and highly selective pan-ErbB kinase inhibitor from a novel aminopyrimidine oxime structural class that blocks the proliferation of epidermal growth factor receptor (EGFR; ErbB1)- and ErbB2-overexpressing cells but does not a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::013ff7bc8f34e49c45e49e5e90b6d746
https://doi.org/10.1124/mol.107.041236
https://doi.org/10.1124/mol.107.041236
Autor:
Niranjan Pandey, Angel R. Fuentes-Pesquera, Eva Binnun, Sigmond G. Johnson, Steven K. Wetter, Sandra Moreno-Mazza, Terry V. Hughes, William V. Murray, Steven A. Middleton, Peter J. Connolly, Ronghui Lin, Mary Adams
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(8)
2,7-Diamino-thiazolo[4,5-d]pyrimidine analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities and inhibited in vitro cellu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::482987d90be9b720be65b623859b5211
https://pubmed.ncbi.nlm.nih.gov/19286381
https://pubmed.ncbi.nlm.nih.gov/19286381
Autor:
Michael P. Neeper, Sandra Moreno-Mazza, Niranjan Pandey, Mary Adams, Peter J. Connolly, Stuart Emanuel, Geoffrey T. Struble, Steven A. Middleton, Angel R. Fuentes-Pesquera, Guozhang Xu, Marta C. Abad, Robert H. Gruninger, Barry A. Springer
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(16)
Members of a novel class of 4-amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones were identified as potent dual ErbB-2/EGFR kinase inhibitors using concept-guided design approach. These compounds inhibited the growth of ErbB-2 over-expressing hum
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f1d0643b2d6b6c6ff9d0573b8bc1be4
https://pubmed.ncbi.nlm.nih.gov/18653333
https://pubmed.ncbi.nlm.nih.gov/18653333
Autor:
Angel R. Fuentes-Pesquera, Sandra Moreno-Mazza, Guozhang Xu, Robert H. Gruninger, Lily Lee Searle, Niranjan Pandey, Marta C. Abad, Peter J. Connolly, Steven A. Middleton, Geoffrey T. Struble, Barry A. Springer, Amanda K. Beck, Lee M. Greenberger, Mary Adams, Terry V. Hughes, Stuart Emanuel, Michael P. Neeper
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(12)
We herein disclose a novel series of 4-aminopyrimidine-5-carbaldehyde oximes that are potent and selective inhibitors of both EGFR and ErbB-2 tyrosine kinases, with IC50 values in the nanomolar range. Structure–activity relationship (SAR) studies e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ccbc47cab1e0393650df86f30153a064
https://pubmed.ncbi.nlm.nih.gov/18508264
https://pubmed.ncbi.nlm.nih.gov/18508264
Autor:
Mary Adams, Linda Jolliffe, Steven A. Middleton, William V. Murray, Steven K. Wetter, Angel R. Fuentes-Pesquera, Ignatius J. Turchi, Yanhua Lu, Niranjan Pandey, Peter J. Connolly, Sandra Moreno-Mazza, Ronghui Lin, Robert H. Gruninger, Stuart Emanuel
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(9)
A novel series of 2,6-diamino-3-acylpyridines were designed and synthesized as cyclin-dependent kinase (CDK) inhibitors. The representative compounds 2r and 11 showed potent CDK1 and CDK2 inhibitory activities and inhibited cellular proliferation in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe8b2ea9ad5dd0df6d72eca07e008bbb
https://pubmed.ncbi.nlm.nih.gov/15837297
https://pubmed.ncbi.nlm.nih.gov/15837297