Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Charles M. Blazey"'
Autor:
John Woolfrey, Craig Stacy Takeuchi, Arthur Plonowski, Kyoko Yamaguchi, Ron Aoyama, Byung Gyu Kim, Anagha Abhijit Joshi, Paul Foster, Sunghoon Ma, Sharmila Rajan, Tae Gon Baik, Naing Aay, Arlyn Arcalas, Charles M. Blazey, Jonah Cannoy, Peter Lamb, Isabelle Lehoux, Chris A. Buhr, Narsimha Munagala, Matthew Sangyup Lee, John M. Nuss, James W. Leahy, Jae Lee, Sergey Epshteyn, Neel Kumar Anand, Nicole Miller, Longcheng Wang, Katherine Lara, Henry Johnson
Publikováno v:
Journal of Medicinal Chemistry. 56:2218-2234
A series of novel, highly potent, selective, and ATP-competitive mammalian target of rapamycin (mTOR) inhibitors based on a benzoxazepine scaffold have been identified. Lead optimization resulted in the discovery of inhibitors with low nanomolar acti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e37d108d9c419238d27ed27c967013b5
https://doi.org/10.1021/jm3007933
https://doi.org/10.1021/jm3007933
Autor:
Sunghoon Ma, Julie Lougheed, Christopher Jaeger, Scott W. Womble, Jean-Claire Limun Manalo, Chris A. Buhr, Longcheng Wang, Wentao Zhang, Kenneth D. Rice, Steven Charles Defina, Abigail R. Kennedy, Timothy S. Heuer, Michael Yakes, Neel Kumar Anand, Tae-Gon Baik, Curtis Jeff Kimo, Joerg Bussenius, Angie I. Kim, Jonathan C. Li, Michael Pack, Csaba J. Peto, Monique Nicoll, Naing Aay, Simona Costanzo, Jae Lee, Garth Joseph Mcgrath, Charles M. Blazey, Tsze H. Tsang, Shiva Malek, Anagha Abhijit Joshi, Arlyn Arcalas, Ping Huang, Larisa Dubenko, Jean-Francois Martini, Katherine Lara, John M. Nuss, Owen Joseph Bowles
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5396-5404
With structural guidance, tropane-derived HTS hits were modified to optimize for HSP90 inhibition and a desirable in vivo profile. Through an iterative SAR development process 12i (XL888) was discovered and shown to reduce HSP90 client protein conten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd3657e6e173629f0f09489df1637838
https://doi.org/10.1016/j.bmcl.2012.07.052
https://doi.org/10.1016/j.bmcl.2012.07.052
Autor:
Jeffry Kimo Curtis, Julie Lougheed, Stefan Engst, Peiwen Yu, Anagha Abhijit Joshi, Elena S. Koltun, Csaba J. Peto, Neel Kumar Anand, Jean-Claire Limun Manalo, Stuart Johnston, Steven Charles Defina, Abigail R. Kennedy, Naing Aay, Kenneth D. Rice, Larisa Dubenko, Tsze H. Tsang, Jean-Francois Martini, Simona Costanzo, John M. Nuss, Angie I. Kim, Owen Joseph Bowles, Joerg Bussenius, Charles M. Blazey
Publikováno v:
ACS Medicinal Chemistry Letters. 3:416-421
The ERK/MAP kinase cascade is a key mechanism subject to dysregulation in cancer and is constitutively activated or highly upregulated in many tumor types. Mutations associated with upstream pathway components RAS and Raf occur frequently and contrib
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a20c73fff311c30e1eae8739e95812e0
https://doi.org/10.1021/ml300049d
https://doi.org/10.1021/ml300049d
Autor:
Kenneth D. Rice, Neel Kumar Anand, Moon Hwan Kim, Jason Jevious Parks, Tsze H. Tsang, Donna T. Le, Larisa Dubenko, Erick Wang Co, Steven Charles Defina, Joerg Bussenius, Lynne Canne-Bannen, David J. Matthews, John M. Nuss, Stefan Engst, Simona Costanzo, Richard George Khoury, A. Douglas Laird, Diva Sze-Ming Chan, Wei Xu, Owen Joseph Bowles, Maurizio Franzini, Vasu Jammalamadaka, Ping Huang, Amy Lew Tsuhako, Yong Wang, David W. Markby, Baili Chen, Morrison B. Mac, Rhett Ronald Klein, Nicole Miller, Charles M. Blazey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2693-2697
Activation of the PI3K/Akt/mTOR kinase pathway is frequently associated with human cancer. Selective inhibition of p70S6Kinase, which is the last kinase in the PI3K pathway, is not sufficient for strong tumor growth inhibition and can lead to activat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84505d7504282ea19f62cf62c9c44716
https://doi.org/10.1016/j.bmcl.2012.03.011
https://doi.org/10.1016/j.bmcl.2012.03.011
Publikováno v:
Tetrahedron Letters. 38:6803-6806
Deuterium labeled methacrylates ( 5,6 ), tiglates ( 10,12 ), and senecioates ( 13,14,16,17 ), important for biosynthetic studies on the synthesis of carboxylic acids in carabid beetles, have been prepared using organocopper-alkyne coupling reactions.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8cd1096ae870cf016fd34ac6c91e1197
https://doi.org/10.1016/s0040-4039(97)01599-2
https://doi.org/10.1016/s0040-4039(97)01599-2
Publikováno v:
The Journal of Organic Chemistry. 62:3236-3241
The absolute stereochemistry of (-)-galbonolide A (1) was assigned by chemical methods. First, 1 was degraded to diol 3. After selective silylation of the primary alcohol, two independent methods were carried out to determine the chirality at C13. Bo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26c6802fdf39ab08abc3671cf474fccb
https://doi.org/10.1021/jo970106l
https://doi.org/10.1021/jo970106l
Autor:
Kenneth D. Rice, Yong Wang, Lynne Canne Bannen, Morrison B. Mac, Vasu Jammalamadaka, Simona Costanzo, Maurizio Franzini, Erick Wang Co, Nicole Miller, Larisa Dubenko, Steven Charles Defina, Joerg Bussenius, Neel Kumar Anand, Douglas Laird, David J. Matthews, John M. Nuss, Jason Jevious Parks, Amy Lew Tsuhako, Rhett Ronald Klein, Donna T. Le, Tsze H. Tsang, Baili Chen, Charles M. Blazey, Moon Hwan Kim, David W. Markby, Richard George Khoury, Wei Xu, Diva Sze-Ming Chan, Owen Joseph Bowles, Stefan Engst, Ping Huang
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(6)
The 70-kDa ribosomal protein S6 kinase (p70S6K) is part of the PI3K/AKT/mTOR pathway and has been implicated in cancer. High throughput screening versus p70S6K led to the identification of aminopyrimidine 3a as active inhibitor. Lead optimization of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82e39bdc172bd771c8f3fbd8b679a60b
https://pubmed.ncbi.nlm.nih.gov/22342124
https://pubmed.ncbi.nlm.nih.gov/22342124
Publikováno v:
ChemInform. 28
The absolute stereochemistry of (−)-galbonolide A (1) was assigned by chemical methods. First, 1 was degraded to diol 3. After selective silylation of the primary alcohol, two independent methods w...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1ff799834132a801c20af0394c8c3e93
https://doi.org/10.1002/chin.199737275
https://doi.org/10.1002/chin.199737275
Publikováno v:
ChemInform. 28
Deuterium labeled methacrylates ( 5,6 ), tiglates ( 10,12 ), and senecioates ( 13,14,16,17 ), important for biosynthetic studies on the synthesis of carboxylic acids in carabid beetles, have been prepared using organocopper-alkyne coupling reactions.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::66b2206da93c23adbbd655be4073fbe2
https://doi.org/10.1002/chin.199751084
https://doi.org/10.1002/chin.199751084
Publikováno v:
The Journal of organic chemistry. 67(1)
The azomethine ylide derived from the condensation of diethyl aminomalonate with paraformaldehyde undergoes 1,3-dipolar cycloadditions with acrylate and propiolate derivatives. Contrary to a previous report, these reactions yield mixtures of regioiso
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fcfd4a636485cc275b0230e150d5f37a
https://pubmed.ncbi.nlm.nih.gov/11777476
https://pubmed.ncbi.nlm.nih.gov/11777476