Edmund Ellsworth , PhD

Publications

Lipid-Based Self-Microemulsion of Niclosamide Achieved Enhanced Oral Delivery and Anti-Tumor Efficacy in Orthotopic Patient-Derived Xenograft of Hepatocellular Carcinoma in Mice. International journal of nanomedicine (2024)

The Novel RXR Agonist MSU-42011 Differentially Regulates Gene Expression in Mammary Tumors of MMTV-Neu Mice International Journal of Molecular Sciences (2023)

Anti-fibrillization effects of sulfonamide derivatives on α-synuclein and hyperphosphorylated tau isoform 1N4R Journal of Molecular Structure (2022)

Small Molecule 20S Proteasome Enhancer Regulates MYC Protein Stability and Exhibits Antitumor Activity in Multiple Myeloma Biomedicines (2022)

Machine Learning Analysis of Cocaine Addiction Informed by DAT, SERT, and NET-Based Interactome Networks Journal of Chemical Theory and Computation (2022)

Structural basis of binding and inhibition of ornithine decarboxylase by 1-amino-oxy-3-aminopropane Biochemical Journal (2021)

The RXR Agonist MSU42011 Is Effective for the Treatment of Preclinical HER2+ Breast Cancer and Kras-Driven Lung Cancer Cancers (2021)

The novel rexinoid MSU-42011 is effective for the treatment of preclinical Kras-driven lung cancer Scientific Reports (2020)

Therapeutic potential of targeting mixed lineage kinases in cancer and inflammation Pharmacology & Therapeutics (2020)

Inhibiting Mycobacterium tuberculosis DosRST Signaling by Targeting Response Regulator DNA Binding and Sensor Kinase Heme ACS Chemical Biology (2020)

Spermine in semen of male sea lamprey acts as a sex pheromone PLOS Biology (2019)

Identification of new MmpL3 inhibitors by untargeted and targeted mutant screens defines MmpL3 domains with differential resistance (2019)

Inhibition of Mycobacterium tuberculosis DosRST two-component regulatory system signaling by targeting response regulator DNA binding and sensor kinase heme (2018)

Review on Abyssomicins: Inhibitors of the Chorismate Pathway and Folate Biosynthesis Molecules (2018)

The discovery of isoxazoline oxime ethers as a new class of ectoparasiticides for the control of Haematobia irritans (horn fly) in cattle Bioorganic & Medicinal Chemistry Letters (2014)

Stereoselective Synthesis of (S)-3-(Methylamino)-3-((R)-pyrrolidin-3-yl)propanenitrile The Journal of Organic Chemistry (2012)

Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring Bioorganic & Medicinal Chemistry Letters (2012)

Physiochemical drug properties associated with in vivo toxicological outcomes Bioorganic & Medicinal Chemistry Letters (2008)

Synthesis and antibacterial activity of the C-7 side chain of 3-aminoquinazolinediones Bioorganic & Medicinal Chemistry Letters (2008)

In Vitro and In Vivo Activities of PD 0305970 and PD 0326448, New Bacterial Gyrase/Topoisomerase Inhibitors with Potent Antibacterial Activities versus Multidrug-Resistant Gram-Positive and Fastidious Organism Groups Antimicrobial Agents and Chemotherapy (2007)

The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents Bioorganic & Medicinal Chemistry Letters (2007)

Structure–activity relationships of 3-aminoquinazolinediones, a new class of bacterial type-2 topoisomerase (DNA gyrase and topo IV) inhibitors Bioorganic & Medicinal Chemistry Letters (2007)

3-Aminoquinazolinediones as a New Class of Antibacterial Agents Demonstrating Excellent Antibacterial Activity Against Wild-Type and Multidrug Resistant Organisms Journal of Medicinal Chemistry (2006)

A facile synthesis of substituted 3-amino-1H-quinazoline-2,4-diones Journal of Heterocyclic Chemistry (2005)

Dicarbonylbis(triphenylphosphine)nickel(0) Encyclopedia of Reagents for Organic Synthesis (2001)

Bromo(o-tolyl)bis(triethylphosphine)nickel(II) Encyclopedia of Reagents for Organic Synthesis (2001)

Synthesis of the novel antibacterial 6,8-dihydroxy-7-propyl-9H-pyrrolo[1,2-b][1,3]-benzoxazin-9-one Tetrahedron Letters (2000)

5,6-Dihydropyran-2-ones Possessing Various Sulfonyl Functionalities:  Potent Nonpeptidic Inhibitors of HIV Protease Journal of Medicinal Chemistry (2000)

Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor Bioorganic & Medicinal Chemistry (1999)

Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety Bioorganic & Medicinal Chemistry Letters (1999)

4-Hydroxy-5,6-Dihydro-2H-pyran-2-ones. 3. Bicyclic and hetero-aromatic ring systems as 3-position scaffolds to bind to S1′ and S2′ of the HIV-1 protease enzyme Bioorganic & Medicinal Chemistry Letters (1999)

Nonpeptidic HIV protease inhibitors: 6-alkyl-5, 6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl, 5-methylphenyl thio) moiety: Antiviral activities and pharmacokinetic properties Bioorganic & Medicinal Chemistry Letters (1999)

Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydro-2-pyranones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety Bioorganic & Medicinal Chemistry Letters (1999)

Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria Chemtracts (1999) (1999)

4-Hydroxy-5,6-dihydropyrones. 2. Potent Non-Peptide Inhibitors of HIV Protease Journal of Medicinal Chemistry (1997)

Synthesis of 5,6-Dihydro-4-hydroxy-2- pyrones as HIV-1 Protease Inhibitors:  The Profound Effect of Polarity on Antiviral Activity Journal of Medicinal Chemistry (1997)

Discovery and optimization of nonpeptide HIV-1 protease inhibitors Bioorganic & Medicinal Chemistry (1996)

Inhibitors of HIV protease: Unique non-peptide active site templates Journal of Molecular Recognition (1996)

A simple procedure for the synthesis of 3‐(substituted‐sulfanyl)‐4‐hydroxy‐6‐substituted‐pyran‐2‐ones Journal of Heterocyclic Chemistry (1994)

Hydrozirconation-transmetalation. A mild, direct route to higher order vinylic cuprates from monosubstituted acetylenes Journal of the American Chemical Society (1990)

On the composition of Yamamoto's reagent: "RCu.cntdot.BF3" Journal of the American Chemical Society (1990)

Higher order cyanocuprates R2Cu(CN)Li2: discrete reagents or lower order lithium cyanide (LiCN) modified Gilman cuprates? Journal of the American Chemical Society (1990)

Ligand exchange between cyanocuprates and allylic stannanes: a novel, direct route to allylic cuprates possessing remarkable reactivity and stability Journal of the American Chemical Society (1990)

New methodology for conjugate additions of allylic ligands to .alpha.,.beta.-unsaturated ketones: synthetic and spectroscopic studies Journal of the American Chemical Society (1990)

A new method for the in situ generation of Cp2Zr(H)Cl (Schwartz' Reagent) Tetrahedron Letters (1990)

Fine tuning the silicon-tin bond: transmetalations forming either trialkylstannyl or trialkylsilyl higher order cyanocuprates The Journal of Organic Chemistry (1989)

Understanding allylic organocuprates: .sigma.- or .pi.-bound reagents? The Journal of Organic Chemistry (1989)

Transmetalation reactions of higher order cyanocuprates: Direct formation of trialkyltin cuprates from tin hydrides which bypasses organolithium intermediates Tetrahedron Letters (1989)

The synthesis of β-Hydroxy-(E)-vinylstannanes using an “in-situ” generated cuprate reagent derived from (E)-bis-(tributylstannyl)ethylene Tetrahedron Letters (1989)

Effects of boron trifluoride etherate on higher order organocuprate reactions: substrate activation or cuprate modification? Journal of the American Chemical Society (1988)

Effects of gengenions on organocuprate reactivity/selectivity: Higher order, mixed lithio- cyanocuprates Tetrahedron Letters (1988)

Unexpected affects of Me3Si-X on reactions of higher order cyanocuprates Tetrahedron Letters (1988)

Design, Synthesis, and Biological Activity of Novel Ornithine Decarboxylase (ODC) Inhibitors.