Search Results - "ALMSTEAD, NEIL G."
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Discovery of Novel Small Molecule Inhibitors of VEGF Expression in Tumor Cells Using a Cell-Based High Throughput Screening Platform
Published in PloS one (16-12-2016)“…Current anti-VEGF (Vascular Endothelial Growth Factor A) therapies to treat various cancers indiscriminately block VEGF function in the patient resulting in…”
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Safety, Tolerability, and Pharmacokinetics of PTC124, a Nonaminoglycoside Nonsense Mutation Suppressor, Following Single- and Multiple-Dose Administration to Healthy Male and Female Adult Volunteers
Published in Journal of clinical pharmacology (01-04-2007)“…Nonsense (premature stop codon) mutations are causative in 5% to 15% of patients with monogenetic inherited disorders. PTC124, a 284‐Dalton 1,2,4‐oxadiazole,…”
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Identification of PTC725, an Orally Bioavailable Small Molecule That Selectively Targets the Hepatitis C Virus NS4B Protein
Published in Antimicrobial Agents and Chemotherapy (01-07-2013)“…OA Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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SMN2 splicing modifiers improve motor function and longevity in mice with spinal muscular atrophy
Published in Science (American Association for the Advancement of Science) (08-08-2014)“…Spinal muscular atrophy (SMA) is a genetic disease caused by mutation or deletion of the survival of motor neuron 1 (SMN1) gene. A paralogous gene in humans,…”
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Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of Dihydroorotate Dehydrogenase with Favorable Pharmaceutical Properties
Published in Molecular cancer therapeutics (01-01-2019)“…PTC299 was identified as an inhibitor of VEGFA mRNA translation in a phenotypic screen and evaluated in the clinic for treatment of solid tumors. To guide…”
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PTC124 targets genetic disorders caused by nonsense mutations
Published in Nature (03-05-2007)“…Nonsense mutations promote premature translational termination and cause anywhere from 5-70% of the individual cases of most inherited diseases. Studies on…”
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Discovery and Optimization of Small Molecule Splicing Modifiers of Survival Motor Neuron 2 as a Treatment for Spinal Muscular Atrophy
Published in Journal of medicinal chemistry (14-07-2016)“…The underlying cause of spinal muscular atrophy (SMA) is a deficiency of the survival motor neuron (SMN) protein. Starting from hits identified in a…”
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Selective Synthesis of 1‑Substituted 4‑Chloropyrazolo[3,4‑d]pyrimidines
Published in Organic letters (19-04-2013)“…Strategies for carrying out the reaction of 4,6-dichloropyrimidine-5-carboxaldehyde with various hydrazines to generate 1-substituted…”
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Design and Synthesis of Piperazine-Based Matrix Metalloproteinase Inhibitors
Published in Journal of medicinal chemistry (10-02-2000)“…A new generation of cyclic matrix metalloproteinase (MMP) inhibitors derived from dl-piperazinecarboxylic acid has been described. The design involves: …”
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Discovery and Optimization of Indolyl-Containing 4‑Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria
Published in Journal of medicinal chemistry (24-05-2018)“…There exists an urgent medical need to identify new chemical entities (NCEs) targeting multidrug resistant (MDR) bacterial infections, particularly those…”
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Design, Synthesis, and Biological Evaluation of Potent Thiazine- and Thiazepine-Based Matrix Metalloproteinase Inhibitors
Published in Journal of medicinal chemistry (04-11-1999)“…The synthesis and enzyme inhibition data for a series of thiazine- and thiazepine-based matrix metalloproteinase (MMP) inhibitors are described. The thiazine-…”
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4-Hydroxy-2-pyridones: Discovery and evaluation of a novel class of antibacterial agents targeting DNA synthesis
Published in Bioorganic & medicinal chemistry letters (15-11-2017)“…[Display omitted] The continued emergence of bacteria resistant to current standard of care antibiotics presents a rapidly growing threat to public health. New…”
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Studies on the mechanism and origin of stereoselective opening of chiral dioxane acetals
Published in Journal of the American Chemical Society (01-10-1991)Get full text
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Discovery of Potent, Achiral Matrix Metalloproteinase Inhibitors
Published in Journal of medicinal chemistry (10-09-1998)Get full text
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Design, Synthesis, and Biological Evaluation of Matrix Metalloproteinase Inhibitors Derived from a Modified Proline Scaffold
Published in Journal of medicinal chemistry (30-12-1999)“…The synthesis and structure−activity relationship (SAR) studies of a series of proline-based matrix metalloproteinase inhibitors are described. The data reveal…”
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Spectroscopic studies on the structure and conformation of Lewis acid-aldehyde complexes
Published in Journal of the American Chemical Society (01-04-1993)Get full text
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On the stereochemical course of the addition of allylsilanes to aldehydes
Published in Tetrahedron (16-09-2012)“…Model compounds 3 and 5 have been studied to determine the orientation of the reacting double bonds in the transition state of the allylmetal–aldehyde…”
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Stereochemical Studies on the Addition of Allylsilanes to Aldehydes. The SE' Component
Published in Journal of organic chemistry (01-09-1994)Get full text
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The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold
Published in Bioorganic & medicinal chemistry letters (06-08-2001)“…A series of carboxylic acids was prepared based on cyclohexylglycine scaffolds and tested for potency as matrix metalloproteinase (MMP) inhibitors. Detailed…”
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