Edmund Ellsworth, PhD
Professor (Fixed-Term) and Medicinal Chemistry Facility Director
Pharmacology & Toxicology
Pharmacology & Toxicology
Research
Colleges
Associations
- MSU Drug Discovery
Facilities
- Medicinal Chemistry Facility
Works
- 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 (2024-03-14)
- The Novel RXR Agonist MSU-42011 Differentially Regulates Gene Expression in Mammary Tumors of MMTV-Neu Mice. International Journal of Molecular Sciences (2023-02-21)
- 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 (2022-04-19)
- Small Molecule 20S Proteasome Enhancer Regulates MYC Protein Stability and Exhibits Antitumor Activity in Multiple Myeloma. Biomedicines (2022-04-19)
- Machine Learning Analysis of Cocaine Addiction Informed by DAT, SERT, and NET-Based Interactome Networks. Journal of Chemical Theory and Computation (2022-04-12)
- Structural basis of binding and inhibition of ornithine decarboxylase by 1-amino-oxy-3-aminopropane. Biochemical Journal (2021-12-10)
- The RXR Agonist MSU42011 Is Effective for the Treatment of Preclinical HER2+ Breast Cancer and Kras-Driven Lung Cancer. Cancers (2021-10-06)
- The novel rexinoid MSU-42011 is effective for the treatment of preclinical Kras-driven lung cancer. Scientific Reports (2020-12-17)
- 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 (2020-01-17)
- Spermine in semen of male sea lamprey acts as a sex pheromone. PLOS Biology (2019-07-09)
- Spermine in semen of male sea lamprey acts as a sex pheromone. PLoS biology (2019-07-09)
- Identification of new MmpL3 inhibitors by untargeted and targeted mutant screens defines MmpL3 domains with differential resistance. (2019-02-28)
- Inhibition of Mycobacterium tuberculosis DosRST two-component regulatory system signaling by targeting response regulator DNA binding and sensor kinase heme. (2018-09-08)
- Review on Abyssomicins: Inhibitors of the Chorismate Pathway and Folate Biosynthesis. Molecules (2018-06-06)
- 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 (2012-05-18)
- 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 (2006-11-01)
- 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 (2001-04-15)
- Bromo(o-tolyl)bis(triethylphosphine)nickel(II). Encyclopedia of Reagents for Organic Synthesis (2001-04-15)
- 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 (2000-03-01)
- 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 (1997-11-01)
- 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 (1997-11-01)
- 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. ()