Zobrazeno 1 - 10
of 62
pro vyhledávání: '"R. Bencsik"'
Autor:
Josef R. Bencsik, Barbara J. Brandhuber, Banka Anna L, Guy Vigers, Nicholas J. Skelton, Stefan D. Gross, Wen-I Wu, Matthew Martinson, Ian S. Mitchell, Susan L. Gloor, Rui Xu, Keith Lee Spencer, Tyler Risom, James F. Blake, Nicholas C. Kallan, Eli M. Wallace, Tony Morales
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2335-2340
We describe the design and synthesis of novel bicyclic spiro sulfonamides as potent Akt inhibitors. Through structure-based rational design, we have successfully improved PKA selectivity of previously disclosed spirochromanes. Representative compound
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d464e766cfa3fd14ff059ee54510b6e
https://doi.org/10.1016/j.bmcl.2011.02.098
https://doi.org/10.1016/j.bmcl.2011.02.098
Autor:
Nicholas J. Skelton, Matthew Martinson, Ian S. Mitchell, Josef R. Bencsik, Susan L. Gloor, Tony Morales, Rui Xu, Keith Lee Spencer, Tyler Risom, Barbara J. Brandhuber, Guy Vigers, Nicholas C. Kallan, Justin W. Heizer, James F. Blake, Wen-I Wu, Stefan D. Gross
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2410-2414
A novel series of spirochromane pan-Akt inhibitors is reported. SAR optimization furnished compounds with improved enzyme potencies and excellent selectivity over the related AGC kinase PKA. Attempted replacement of the phenol hinge binder provided c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05a61cc2ceaf948857e1551953322040
https://doi.org/10.1016/j.bmcl.2011.02.073
https://doi.org/10.1016/j.bmcl.2011.02.073
Autor:
Keith Lee Spencer, Tyler Risom, Guy Vigers, Nicholas J. Skelton, Stefan D. Gross, Nicholas C. Kallan, Josef R. Bencsik, James F. Blake, Matthew Martinson, Ian S. Mitchell, Rui Xu, Richard Woessner, Tony Morales, Susan L. Gloor, Dengming Xiao, Barbara J. Brandhuber
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5607-5612
The discovery and optimization of a series of pyrrolopyrimidine based protein kinase B (Pkb/Akt) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent inhibition of all three Akt isoforms and knoc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77658a908ccac79354e5f6c50c34c693
https://doi.org/10.1016/j.bmcl.2010.08.053
https://doi.org/10.1016/j.bmcl.2010.08.053
Publikováno v:
Organic Letters. 5:2727-2730
[reaction: see text] The bicyclocondensation of 3-aza-1,5-ketoacids and amino alcohols furnished novel oxazolo[3,2-a]pyrazin-5-one scaffolds possessing angular, ring junction substituents in high yield with excellent levels of substrate-based diaster
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee92df1cbc2ed9a9c3197d92e47a274a
https://doi.org/10.1021/ol030065h
https://doi.org/10.1021/ol030065h
Autor:
Jun Li, Dengming Xiao, Eli M. Wallace, Brian Safina, Deepak Sampath, Christine Chabot, Matthew Martinson, Ian S. Mitchell, Barbara J. Brandhuber, Jason Oeh, Rui Xu, Steven Do, Leslie Lee, Jun Liang, Susan L. Gloor, Birong Zhang, Kui Lin, Stephen T. Schlachter, Nicholas J. Skelton, Brian Lee, Bianca M. Liederer, Richard Woessner, Guy Vigers, James F. Blake, Josef R. Bencsik, Banka Anna L, Nicholas C. Kallan, Keith Lee Spencer
Publikováno v:
Journal of medicinal chemistry. 55(18)
The discovery and optimization of a series of 6,7-dihydro-5H-cyclopenta[d]pyrimidine compounds that are ATP-competitive, selective inhibitors of protein kinase B/Akt is reported. The initial design and optimization was guided by the use of X-ray stru
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc7a361953c152bbaff8d2beb18d5c35
https://pubmed.ncbi.nlm.nih.gov/22934575
https://pubmed.ncbi.nlm.nih.gov/22934575
Publikováno v:
Spektrum der Augenheilkunde. 8:272-275
Unser Ziel war das Pseudoexfoliationsglaukom (unilateral 29, bilateral 21) bei der Entdeckung mit dem primaren chronischen Offenwinkelglaukom (50) zu vergleichen. In der Gruppe der Pseudoexfoliationsglaukome wo das Durchschnittsalter um etwa 10 Jahre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0c28b676e2ab8081afe13c829278b200
https://doi.org/10.1007/bf03163717
https://doi.org/10.1007/bf03163717
Publikováno v:
ChemInform. 31
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::21936363209ffaed6a72e9b0d8b9d2ab
https://doi.org/10.1002/chin.200005261
https://doi.org/10.1002/chin.200005261
Publikováno v:
Organic Letters. 1:1483-1485
The enantioselective total synthesis of the Streptomyces metabolite (−)-LL-C10037α has been accomplished in 10 steps and 20% overall yield. An early chiral intermediate was resolved with Candida rugosa lipase to provide (+)-5 with an enantiomeric
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6e0297f9a94462379d37d35cb650c5a8
https://doi.org/10.1021/ol991038n
https://doi.org/10.1021/ol991038n
Publikováno v:
Journal of combinatorial chemistry. 9(6)
Due to their diverse range of biological activities, imidazoheterocycles are recognized as privileged structures making these structural motifs attractive targets for library preparation. We report herein the synthesis of a sizable collection of imid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e17b64745b7d0cc2d71d266713668453
https://pubmed.ncbi.nlm.nih.gov/17824665
https://pubmed.ncbi.nlm.nih.gov/17824665
Publikováno v:
ChemInform. 34
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::04a9b1376dff111c2ec63b7a36bc44c4
https://doi.org/10.1002/chin.200349137
https://doi.org/10.1002/chin.200349137