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- Publications
- Influence
N-(Pivaloyloxy)alkoxy-carbonyl Prodrugs of the Glutamine Antagonist 6-Diazo-5-oxo-l-norleucine (DON) as a Potential Treatment for HIV Associated Neurocognitive Disorders.
- Michael T. Nedelcovych, Lukáš Tenora, +17 authors B. Slusher
- Chemistry, Medicine
- Journal of medicinal chemistry
- 14 August 2017
Aberrant excitatory neurotransmission associated with overproduction of glutamate has been implicated in the development of HIV-associated neurocognitive disorders (HAND). The glutamine antagonist… Expand
Targeting glutamine metabolism enhances tumor specific immunity by modulating suppressive myeloid cells.
- M. Oh, I. Sun, +17 authors J. Powell
- Medicine, Chemistry
- The Journal of clinical investigation
- 23 April 2020
Myeloid cells comprise a major component of the tumor-microenvironment (TME) promoting tumor growth and immune evasion. By employing a novel small molecule inhibitor of glutamine metabolism, not only… Expand
JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress
- X. Zhu, Michael T. Nedelcovych, +15 authors A. Kamiya
- Medicine
- Neuropsychopharmacology
- 1 March 2019
There are a number of clinically effective treatments for stress-associated psychiatric diseases, including major depressive disorder (MDD). Nonetheless, many patients exhibit resistance to… Expand
Discovery of 6-Diazo-5-oxo-l-norleucine (DON) Prodrugs with Enhanced CSF Delivery in Monkeys: A Potential Treatment for Glioblastoma.
- R. Rais, A. Jancarik, +14 authors B. Slusher
- Chemistry, Medicine
- Journal of medicinal chemistry
- 6 September 2016
The glutamine antagonist 6-diazo-5-oxo-l-norleucine (DON, 1) has shown robust anticancer efficacy in preclinical and clinical studies, but its development was halted due to marked systemic… Expand
Discovery of a para-Acetoxy-benzyl Ester Prodrug of a Hydroxamate-Based Glutamate Carboxypeptidase II Inhibitor as Oral Therapy for Neuropathic Pain.
- R. Rais, J. Vávra, +13 authors B. Slusher
- Chemistry, Medicine
- Journal of medicinal chemistry
- 18 September 2017
4-Carboxy-α-[3-(hydroxyamino)-3-oxopropyl]-benzenepropanoic acid 1 is a potent hydroxamate-based inhibitor of glutamate carboxypeptidase II. In an attempt to improve its poor oral pharmacokinetics,… Expand
Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA).
- P. Majer, A. Jancarik, +8 authors B. Slusher
- Chemistry, Medicine
- Journal of medicinal chemistry
- 10 March 2016
2-Phosphonomethylpentanedioic acid (1, 2-PMPA) is a potent inhibitor of glutamate carboxypeptidase II which has demonstrated robust neuroprotective efficacy in many neurological disease models.… Expand
N-Substituted Prodrugs of Mebendazole Provide Improved Aqueous Solubility and Oral Bioavailability in Mice and Dogs.
- Sarah C. Zimmermann, T. Tichý, +12 authors R. Rais
- Chemistry, Medicine
- Journal of medicinal chemistry
- 12 April 2018
Mebendazole (MBZ) was developed as a broad-spectrum anthelmintic but has recently shown efficacy as an anticancer agent. The use of MBZ for cancer, however, is challenging due to its poor solubility… Expand
The Synthesis of Two Regioisomeric Aldehydes with a Tetrahydrobenzo[b]thiophene Scaffold and Their Application in Solvent-Free Intramolecular 1,3-Dipolar Cycloaddition Reactions
- Lukáš Tenora, S. Man, E. V. D. Berge, M. Potáček
- Chemistry
- 26 April 2016
The paper describes the synthesis of two regioisomeric 2-amino-3-formyl- and 3-amino-2-formyl-substituted derivatives of tetrahydrobenzo[ b ]thiophene and their subsequent thermally initiated… Expand
A new and facile synthesis of methyl 3-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylate
- Lukáš Tenora, Marian Buchlovič, S. Man, M. Potáček
- Chemistry
- 19 January 2011
A four-step synthesis of methyl 3-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylate from commercially available starting materials is presented.
Dihydropyrrolo[1,2-b]pyrazoles: withasomnine and related compounds
- J. Galeta, Lukáš Tenora, S. Man, M. Potáček
- Chemistry
- 26 August 2013
In the paper we indicate the increasing importance of
derivatives containing a dihydropyrrolo[1,2-b]pyrazole (DPP)
core. We try to show our synthetic approach based on an
improved Kulinkovich method… Expand