Search Results - "Verheijen, Jeroen C."

Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR) by KAPLAN, Joshua, VERHEIJEN, Jeroen C, BROOIJMANS, Natasja, TORAL-BARZA, Lourdes, HOLLANDER, Irwin, YU, Ker, ZASK, Arie

“…The morpholine hinge-region binding group on a series of pyrazolopyrimidine and thienopyrimidine mammalian target of rapamycin (mTOR) inhibitors was replaced…”
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Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β‑Lactamases by Durand-Réville, Thomas F, Comita-Prevoir, Janelle, Zhang, Jing, Wu, Xiaoyun, May-Dracka, Tricia L, Romero, Jan Antoinette C, Wu, Frank, Chen, April, Shapiro, Adam B, Carter, Nicole M, McLeod, Sarah M, Giacobbe, Robert A, Verheijen, Jeroen C, Lahiri, Sushmita D, Sacco, Michael D, Chen, Yu, O’Donnell, John P, Miller, Alita A, Mueller, John P, Tommasi, Rubén A

“…Multidrug resistant Gram-negative bacterial infections are an increasing public health threat due to rapidly rising resistance toward β-lactam antibiotics. The…”
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Morpholine Derivatives Greatly Enhance the Selectivity of Mammalian Target of Rapamycin (mTOR) Inhibitors by Zask, Arie, Kaplan, Joshua, Verheijen, Jeroen C, Richard, David J, Curran, Kevin, Brooijmans, Natasja, Bennett, Eric M, Toral-Barza, Lourdes, Hollander, Irwin, Ayral-Kaloustian, Semiramis, Yu, Ker

“…Dramatic improvements in mTOR-targeting selectivity were achieved by replacing morpholine in pyrazolopyrimidine inhibitors with bridged morpholines. Analogues…”
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Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabicyclo[3.2.1 ]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K by VERHEIJEN, Jeroen C, YU, Ker, TORAL-BARZA, Lourdes, HOLLANDER, Irwin, ZASK, Arie

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ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines by Zask, Arie, Verheijen, Jeroen C, Curran, Kevin, Kaplan, Joshua, Richard, David J, Nowak, Pawel, Malwitz, David J, Brooijmans, Natasja, Bard, Joel, Svenson, Kristine, Lucas, Judy, Toral-Barza, Lourdes, Zhang, Wei-Guo, Hollander, Irwin, Gibbons, James J, Abraham, Robert T, Ayral-Kaloustian, Semiramis, Mansour, Tarek S, Yu, Ker

“…The mammalian target of rapamycin (mTOR), a central regulator of growth, survival, and metabolism, is a validated target for cancer therapy. Rapamycin and its…”
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Discovery of 2-arylthieno[3,2- d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K by Verheijen, Jeroen C., Yu, Ker, Toral-Barza, Lourdes, Hollander, Irwin, Zask, Arie

“…Introduction of bridged morpholine and ureidophenyl on moderately potent thienopyrimidine dual PI3K/mTOR inhibitors led to excellent mTOR potency and…”
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Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituent by Curran, Kevin J., Verheijen, Jeroen C., Kaplan, Joshua, Richard, David J., Toral-Barza, Lourdes, Hollander, Irwin, Lucas, Judy, Ayral-Kaloustian, Semiramis, Yu, Ker, Zask, Arie

“…Combination of a 1-cyclohexyl ketal group with a 2,6-ethylene bridged morpholine in the 4-position and a ureidophenyl group in the 6-positon of the…”
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Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: Discovery of highly potent and selective analogs with improved human microsomal stability by Richard, David J., Verheijen, Jeroen C., Curran, Kevin, Kaplan, Joshua, Toral-Barza, Lourdes, Hollander, Irwin, Lucas, Judy, Yu, Ker, Zask, Arie

“…A series of pyrazolopyrimidine mTOR inhibitors which contain basic amines or polar substituents attached to the 6-arylureidophenyl moiety demonstrate enhanced…”
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Triazines incorporating ( R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kα by Richard, David J., Verheijen, Jeroen C., Yu, Ker, Zask, Arie

“…Potent inhibitors of the mammalian target of rapamycin (mTOR) which contain the triazine scaffold and the ( R)-3-methyl morpholine moiety have been identified…”
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Recent advances in the discovery of small-molecule ATP competitive mTOR inhibitors: a patent review by Zask, Arie, Verheijen, Jeroen C, Richard, David J

“…The mammalian target of rapamycin (mTOR) is a protein kinase and a key component of the PI3K/Akt/mTOR signaling pathway, and is deregulated in half of all…”
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Discovery of 4-Morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as Highly Potent and Selective ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin (mTOR): Optimization of the 6-Aryl Substituent by Verheijen, Jeroen C, Richard, David J, Curran, Kevin, Kaplan, Joshua, Lefever, Mark, Nowak, Pawel, Malwitz, David J, Brooijmans, Natasja, Toral-Barza, Lourdes, Zhang, Wei-Guo, Lucas, Judy, Hollander, Irwin, Ayral-Kaloustian, Semiramis, Mansour, Tarek S, Yu, Ker, Zask, Arie

“…Design and synthesis of a series of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as potent and selective inhibitors of the mammalian target of rapamycin…”
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Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors by Zask, Arie, Verheijen, Jeroen C., Richard, David J., Kaplan, Joshua, Curran, Kevin, Toral-Barza, Lourdes, Lucas, Judy, Hollander, Irwin, Yu, Ker

“…Incorporation of bridged morpholines in monocyclic triazine PI3K/mTOR inhibitors gave compounds with increased mTOR selectivity relative to the corresponding…”
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2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: Optimization of human microsomal stability by Verheijen, Jeroen C., Richard, David J., Curran, Kevin, Kaplan, Joshua, Yu, Ker, Zask, Arie

“…Isosteric replacement of one of the 3,5-ethylene-bridged morpholines in triazine mTOR inhibitors led to significant improvements in human microsomal stability,…”
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Discovery of Potent and Selective Inhibitors of the Mammalian Target of Rapamycin (mTOR) Kinase by Nowak, Pawel, Cole, Derek C, Brooijmans, Natasja, Bursavich, Matthew G, Curran, Kevin J, Ellingboe, John W, Gibbons, James J, Hollander, Irwin, Hu, YongBo, Kaplan, Joshua, Malwitz, David J, Toral-Barza, Lourdes, Verheijen, Jeroen C, Zask, Arie, Zhang, Wei-Guo, Yu, Ker

“…The mammalian target of rapamycin (mTOR) is a central regulator of cell growth, metabolism, and angiogenesis and an emerging target in cancer research. High…”
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New antibacterial agents: patent applications published in 2011 by Keating, Thomas A, Lister, Troy, Verheijen, Jeroen C

“…This article reviews 101 patent applications published in 2011 that disclosed small-molecule antibacterials and reported bacterial growth inhibition, in which…”
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4,5-Disubstituted 6‑Aryloxy-1,3-dihydrobenzo[c][1,2]oxaboroles Are Broad-Spectrum Serine β‑Lactamase Inhibitors by McKinney, David C, Zhou, Fei, Eyermann, Charles J, Ferguson, Andrew D, Prince, D. Bryan, Breen, John, Giacobbe, Robert A, Lahiri, Sushmita, Verheijen, Jeroen C

“…Bacterially expressed β-lactamases are rapidly eroding the clinical utility of the important β-lactam class of antibacterials, significantly impairing our…”
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Alkylidene Oxapenem β‑Lactamase Inhibitors Revisited: Potent Broad Spectrum Activity but New Stability Challenges by Miller, Matthew D, Kale, Manoj, Reddy, Kishore, Tentarelli, Sharon, Zambrowski, Mark, Zhang, Minli, Palmer, Tiffany, Breen, John, Lahiri, Sushmita, Shirude, Pravin S, Verheijen, Jeroen C

“…We present a comprehensive study of C6-alkylidene containing oxapenems. We show that this class of β-lactamase inhibitors possesses an unprecedented spectrum…”
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Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition by Verheijen, Jeroen C., Wiig, Kjesten A., Du, Shoucheng, Connors, Stacie L., Martin, Ashley N., Ferreira, Jennifer P., Slepnev, Vladimir I., Kochendörfer, Ulrike

“…Upon inhibition of cholinesterase by 4a–d, pharmacologically active amines are released. Conjugation of the phenol derived from rivastigmine with amphetamines…”
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New antibacterial agents: patent applications published in 2010 by Stokes, Suzanne S, Morningstar, Marshall, Kocis, Helena, Verheijen, Jeroen C

“…This review summarizes patent applications from 2010 for small molecules for which there is a claim of antibacterial activity. The primary criterion for…”
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Transition Metal Derivatives of Peptide Nucleic Acid (PNA) OligomersSynthesis, Characterization, and DNA Binding by Verheijen, Jeroen C, van der Marel, Gijs A, van Boom, Jacques H, Metzler-Nolte, Nils

“…This work describes the first automated solid-phase synthesis of metal derivatives of peptide nucleic acid (PNA) oligomers and their interaction with DNA and…”
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