Search Results - "Harried, Scott"
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Discovery of TRPM8 Antagonist (S)‑6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine
Published in Journal of medicinal chemistry (27-09-2018)“…Transient-receptor-potential melastatin 8 (TRPM8), the predominant mammalian cold-temperature thermosensor, is a nonselective cation channel expressed in a…”
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Extracellular Antibody Drug Conjugates Exploiting the Proximity of Two Proteins
Published in Molecular therapy (01-10-2016)“…The human Na+/K+-ATPase (NKA) is a plasma membrane ion pump that uses ATP to help maintain the resting potential of all human cells. Inhibition of the NKA…”
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Design and Preparation of a Potent Series of Hydroxyethylamine Containing β-Secretase Inhibitors That Demonstrate Robust Reduction of Central β-Amyloid
Published in Journal of medicinal chemistry (08-11-2012)“…A series of potent hydroxyethyl amine (HEA) derived inhibitors of β-site APP cleaving enzyme (BACE1) was optimized to address suboptimal pharmacokinetics and…”
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Unified Total Synthesis of Pteriatoxins and Their Diastereomers
Published in Journal of the American Chemical Society (14-06-2006)“…A unified total synthesis is reported to access all of the possible diastereomers of pteriatoxins A−C, with the use of an intramolecular Diels−Alder reaction…”
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Design and Synthesis of Potent, Orally Efficacious Hydroxyethylamine Derived β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors
Published in Journal of medicinal chemistry (08-11-2012)“…We have previously shown that hydroxyethylamines can be potent inhibitors of the BACE1 enzyme and that the generation of BACE1 inhibitors with CYP 3A4…”
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Stereoselective Synthesis of anti-N-Protected 3-Amino-1,2-epoxides by Nucleophilic Addition to N-tert-Butanesulfinyl Imine of a Glyceraldehyde Synthon
Published in Journal of organic chemistry (21-08-2009)“…A di-O-TBS protected glyceraldehyde synthon was condensed with Ellman’s reagent to form a bench-stable N-tert-butanesulfinyl imine 6, which served as a common…”
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A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase
Published in ACS medicinal chemistry letters (08-11-2012)“…β-Secretase inhibitors are potentially disease-modifying treatments for Alzheimer's disease. Previous efforts in our laboratory have resulted in…”
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Total Synthesis of the Potent Microtubule-Stabilizing Agent (+)-Discodermolide
Published in Journal of organic chemistry (22-08-2003)“…The total synthesis of the potent microtubule-stabilizing, antimitotic agent (+)-discodermolide is described. The convergent synthetic strategy takes advantage…”
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Total Synthesis of (−)-Discodermolide: An Application of a Chelation-Controlled Alkylation Reaction
Published in Journal of organic chemistry (05-09-1997)Get full text
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Abstract 1202: Target identification for a new type of ADC
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Abstract Purpose: To explore the mechanism of action of a potent new type of antibody drug conjugate (ADC) called Extracellular Drug Conjugates or EDCs…”
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Abstract A125: Antibody targeted steroids for the treatment of cancer
Published in Molecular cancer therapeutics (01-12-2015)“…Abstract Purpose: The cardiac glycoside family of steroidal drugs has been shown to possess novel and potent antitumor activities in rodents. Yet most likely…”
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Abstract 2964: An anti-CD20 extracellular antibody-drug conjugate for the treatment of B-cell malignancies
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Abstract Purpose: CD20 is known to be a therapeutic antibody drug target as it is expressed on the surface of most B-cell neoplasms. Here, we assessed the…”
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An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities
Published in ACS medicinal chemistry letters (12-02-2015)“…BACE1 inhibition to prevent Aβ peptide formation is considered to be a potential route to a disease-modifying treatment for Alzheimer’s disease. Previous…”
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A total synthesis of (-)-discodermolide
Published 01-01-1998“…The potent microtubule-stabilizing agent discodermolide is a polypropionate-derived marine natural product with antitumor activity similar to that of taxol. A…”
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Dissertation