R. Magolda

发表

Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase*

F. Hobbs, E. Manos, R. Copeland, 1998, The Journal of Biological Chemistry.

MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.

J. Wityak, G. Trainor, F. Hobbs, 1998, Bioorganic & medicinal chemistry letters.

Discovery of γ-Lactam Hydroxamic Acids as Selective Inhibitors of Tumor Necrosis Factor α Converting Enzyme: Design, Synthesis, and Structure−Activity Relationships

Chen Lihua, Zelda R. Wasserman, Karl D. Hardman, 2002 .

Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.

Rajiv Chopra, Iwan Gunawan, Jim Turner, 2010, Journal of medicinal chemistry.

Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.

Robert Steffan, Anna Wilhelmsson, T. Bonn, 2008, Journal of medicinal chemistry.

Chemistry and pharmacokinetics of diarylthiophenes and terphenyls as selective COX-2 inhibitors

R. Copeland, R. Magolda, J. Trzăskos, 1996 .

Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

R. Magolda, J. Trzăskos, M. Covington, 2003, Bioorganic & medicinal chemistry letters.

Heteroatom- and carbon-linked biphenyl analogs of Brequinar as immunosuppressive agents.

R. Copeland, B. Jaffee, R. Magolda, 1998, Bioorganic & medicinal chemistry letters.

Side effects of brequinar and brequinar analogues, in combination with cyclosporine, in the rat.

B. Jaffee, R. Magolda, H. Schuurman, 1998, Toxicology.

Aggrecanase: A Target for the Design of Inhibitors of Cartilage Degradation

R. Magolda, J. Trzăskos, C. Decicco, 1999, Annals of the New York Academy of Sciences.

Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.

R. Magolda, M. Covington, C. Decicco, 2001, Journal of medicinal chemistry.

Lanosterol 14 alpha-methyl demethylase. Isolation and characterization of the third metabolically generated oxidative demethylation intermediate.

R. Magolda, J. Trzăskos, B. Larsen, 1991, The Journal of biological chemistry.

COMPARISON OF SNAKE VENOM REPROLYSIN AND MATRIX METALLOPROTEINASES AS MODELS OF TNF-α CONVERTING ENZYME

J. Fox, G. Davis, R. Copeland, 1997 .

Vinylogous hydroxamic acids: 5-lipoxygenase inhibitors

S. Wright, R. Magolda, D. Pinto, 1992 .

Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.

D. J. Nelson, K. D. Hardman, R. Copeland, 2001, Journal of medicinal chemistry.

Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).

B. Tomczuk, R. DesJarlais, D. Ryan, 2008, Bioorganic & medicinal chemistry letters.

Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.

R. Magolda, J. Trzăskos, M. Covington, 2003, Bioorganic & medicinal chemistry letters.

Purification and cloning of aggrecanase-1: a member of the ADAMTS family of proteins.

R. Wynn, R. Copeland, R. Wynn, 1999, Science.

Isothiazolones interfere with normal matrix metalloproteinase activation and inhibit cartilage proteoglycan degradation.

S. Wright, R. Magolda, J. Trzăskos, 1996, The Biochemical journal.

Novel Synthesis of Potent Site-Specific Phospholipase A2 Inhibitors

R. Magolda, W. Ripka, M. Rudnick, 1985 .

Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides.

G. Welmaker, R. Bhat, P. Bodine, 2009, Journal of medicinal chemistry.

Prostaglandin I2 as a potentiator of acute inflammation in rats.

K. Nicolaou, R. Magolda, S. Kurozumi, 1978, Prostaglandins.

Carbocyclic thromboxane A2: aggrevation of myocardial ischemia by a new synthetic thromboxane A2 analog.

E. Smith, R. Magolda, A. Lefer, 1981, Prostaglandins.

Amide surrogates of matrix metalloproteinase inhibitors : Urea and sulfonamide mimics

D. J. Nelson, R. Magolda, M. Covington, 1997 .

Synthesis and biological properties of pinane-thromboxane A2, a selective inhibitor of coronary artery constriction, platelet aggregation, and thromboxane formation.

E. F. Smith, A. M. Lefer, R. Magolda, 1979, Proceedings of the National Academy of Sciences of the United States of America.

Protective effects of a novel thromboxane analog in lethal traumatic shock.

R. Magolda, H. Araki, A. Lefer, 1979, Prostaglandins and medicine.

JPET #152975 1 TITLE: GSI-953 (begacestat): A novel, selective thiophene sulfonamide inhibitor of APP γ-secretase for the treatment of Alzheimer’s disease

T. Comery, B. Harrison, M. Pangalos, 2009 .

SYNTHESIS AND BIOLOGICAL PROPERTIES OF PROSTACYCLINS AND PROSTAGLANDIN ENDOPEROXIDE ANALOGS

K. Nicolaou, R. Magolda, W. E. Barnette, 1979 .

Microsomal enzymes of cholesterol biosynthesis from lanosterol. Solubilization and purification of steroid 8-isomerase.

Y. Paik, R. Magolda, J. Billheimer, 1986, The Journal of biological chemistry.

2,5-Diarylisothiazolone: novel inhibitors of cytokine-induced cartilage destruction.

S. Wright, J. Williams, R. Magolda, 1996, Bioorganic & medicinal chemistry.

The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.

M. Day, T. Comery, S. Grauer, 2010, Journal of medicinal chemistry.

Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK).

Renee L DesJarlais, Mark R Player, R. DesJarlais, 2003, Bioorganic & medicinal chemistry letters.

Organoselenium-induced ring closures. Stereoselective synthesis of cyclic .alpha.,.beta.-unsaturated sulfoxides, sulfones, and sulfides and synthesis of 6,9-sulfoxa-5(E)- and -5(Z)-prostacyclin, 6,9-sulfo-5(E)- and -5(Z)-prostacyclin, 6,9-sulfo-6.alpha.- and -6.beta.-4(E)-isoprostacyclin, and 6,9-th

K. Nicolaou, R. Magolda, W. E. Barnette, 1978 .

Organoselenium-based synthesis of oxygen-containing prostacyclins

K. Nicolaou, R. Magolda, W. E. Barnette, 1981 .

Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists.

A. Robichaud, R. Magolda, H. Elokdah, 2007, Bioorganic & medicinal chemistry.

Phenylselenoetherification. A highly efficient cyclization process for the synthesis of oxygen- and sulfur-heterocycles

K. Nicolaou, R. Magolda, M. Joullié, 1980 .

Synthesis of (5Z)- and (5E)-6,9-thiaprostacyclins

K. Nicolaou, R. Magolda, W. E. Barnette, 1981 .

(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.

Raymond J. Unwalla, P. Bodine, R. Magolda, 2009, Journal of medicinal chemistry.

Total synthesis of ionophore antibiotic X-14547A

K. Nicolaou, R. Magolda, R. Dolle, 1985 .

Carbocyclic thromboxane A2

K. Nicolaou, R. Magolda, D. Claremon, 1980 .

Total synthesis of carboprostacyclin, a stable and biologically active analogue of prostacyclin (PGI2)

K. Nicolaou, S. P. Seitz, R. Magolda, 1978 .

Recent Advances in Inflammatory and Immunological Diseases: Focus on Arthritis Therapy

J. Skotnicki, R. Magolda, R. Newton, 2007 .

Total synthesis of ionophore antibiotic X-14547A

K. Nicolaou, R. Magolda, R. Dolle, 1985 .

Total synthesis of ionophore antibiotic X-14547A. 2. Coupling of the tetrahydropyran and tetrahydroindan systems and construction of the butadienyl and ketopyrrole moieties

K. Nicolaou, R. Magolda, D. Claremon, 1981 .

Design, Synthesis, and Evaluation of Benzothiadiazepine Hydroxamates as Selective Tumor Necrosis Factor-α Converting Enzyme Inhibitors

S. Mandlekar, K. D. Hardman, R. Magolda, 2003 .

6,9-thiaprostacyclin. A stable and biologically potent analogue of prostacyclin (PGI2)

G. Gasic, K. Nicolaou, R. Magolda, 1977, Journal of the American Chemical Society.

Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.

B. Jaffee, R. Magolda, J. Trzăskos, 2001, Journal of Medicinal Chemistry.

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.

Xiaohua He, John Roderick, R. Magolda, 2003, Bioorganic & medicinal chemistry letters.

Substrate-based inhibitors of lanosterol 14 alpha-methyl demethylase: I. Assessment of inhibitor structure-activity relationship and cholesterol biosynthesis inhibition properties.

S S Ko, M. Favata, R. Magolda, 1995, Biochemistry.

Modulation of 3-hydroxy-3-methylglutaryl-CoA reductase by 15 alpha-fluorolanost-7-en-3 beta-ol. A mechanism-based inhibitor of cholesterol biosynthesis.

M. Favata, R. Magolda, J. Trzăskos, 1993, The Journal of biological chemistry.

[12] Synthesis of α-isopropylmalate, β-isopropylmalate, and dimethylcitraconate

R. Magolda, J. Schloss, M. Emptage, 1988 .

Inhibition of cartilage breakdown by isothiazolones

M. Abelman, S. Wright, R. Magolda, 1993 .

Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.

S. Mandlekar, K. D. Hardman, R. Magolda, 2003, Journal of medicinal chemistry.

Dissociation of vasoconstrictor and platelet aggregatory activities of thromboxane by carbocyclic thromboxane A2, a stable analog of thromboxane A2.

A. M. Lefer, E. Smith, R. Magolda, 1980, Proceedings of the National Academy of Sciences of the United States of America.

Design and synthesis of conformationally restricted phospholipids as phospholipase A2 inhibitors

R. Magolda, W. Galbraith, R. L. Magolda, 1989, Journal of cellular biochemistry.

Aggrecan Protects Cartilage Collagen from Proteolytic Cleavage*

R. Copeland, R. Magolda, J. Trzăskos, 2003, Journal of Biological Chemistry.

Simple efficient synthesis of prostacyclin (PGI2)1

G. Gasic, K. Nicolaou, R. Magolda, 1977 .

The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase.

Jack Parker Davis, R. Copeland, R. Magolda, 1996, Biochemistry.

Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.

D. Ryan, G. Roth, M. Kashem, 2008, Bioorganic & medicinal chemistry letters.

Begacestat (GSI-953): A Novel, Selective Thiophene Sulfonamide Inhibitor of Amyloid Precursor Protein γ-Secretase for the Treatment of Alzheimer's Disease

T. Comery, B. Harrison, M. Pangalos, 2009, Journal of Pharmacology and Experimental Therapeutics.

Inhibition of mitogen-activated protein kinase kinase blocks T cell proliferation but does not induce or prevent anergy.

B. Jaffee, M. Favata, R. Magolda, 1998, Journal of immunology.

Induce or Prevent Anergy Kinase Blocks T Cell Proliferation But Does Not Inhibition of Mitogen-Activated Protein Kinase

B. Jaffee, M. Favata, R. Magolda, 1998 .

Cloning and Characterization of ADAMTS11, an Aggrecanase from the ADAMTS Family*

R. Wynn, R. Copeland, Y. Itoh, 1999, The Journal of Biological Chemistry.

RAPID AND EASY PREPARATION OF PROSTACYCLIN

G. Gasic, K. Nicolaou, R. Magolda, 1977, The Lancet.

Beneficial actions of a new thromboxane analog in traumatic shock.

R. Magolda, H. Araki, A. Lefer, 1980, Advances in prostaglandin and thromboxane research.

Inhibition of MAP kinase kinase prevents cytokine and prostaglandin E2 production in lipopolysaccharide-stimulated monocytes.

M. Favata, A. J. Daulerio, R. Magolda, 1998, Journal of immunology.

Preservation of ischemic myocardium by pinane thromboxane A2.

A. M. Lefer, K. Schrör, E. Smith, 1980, The American journal of physiology.

Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium.

R. Copeland, B. Jaffee, W. Pitts, 1998, Bioorganic & medicinal chemistry letters.

Immunosuppressive structure-activity relationships of Brequinar and related cinchoninic acid derivatives

R. Copeland, B. Jaffee, W. Pitts, 1995 .

Enhanced clearance of Aβ in brain by sustaining the plasmin proteolysis cascade

T. Comery, A. Robichaud, M. Pangalos, 2008, Proceedings of the National Academy of Sciences.

Effects of brequinar sodium on cynomolgus monkeys: immunosuppression and pharmacokinetics.

B. Jaffee, R. Magolda, D. Cramer, 1993, Transplantation proceedings.

Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities

M. Pangalos, B. Ruan, J. Skotnicki, 2008, Proceedings of the National Academy of Sciences.

Discovery and optimization of p38 inhibitors via computer-assisted drug design.

Angela Berry, Jinhua J. Song, Ming-Hong Hao, 2007, Journal of medicinal chemistry.

Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors.

J. Wityak, G. Trainor, R. Copeland, 2004, Bioorganic & medicinal chemistry letters.

Lipopolysaccharide-Stimulated Monocytes Production in 2 Cytokine and Prostaglandin E Inhibition of MAP Kinase Kinase Prevents

M. Favata, A. J. Daulerio, R. Magolda, 1998 .

Design, Synthesis, and Structure−Activity Relationships of Macrocyclic Hydroxamic Acids That Inhibit Tumor Necrosis Factor α Release in Vitro and in Vivo

Chen Lihua, Robert A. Copeland, David J. Nelson, 2001 .

Discovery of potent and selective PKC-θ inhibitors

Mario G. Cardozo, Mohammed A. Kashem, Carol Ann Homon, 2007 .

Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.

T. Comery, K. Fan, B. Harrison, 2008, Journal of medicinal chemistry.

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.

R. Magolda, J. Trzăskos, K. Vaddi, 2004, Bioorganic & medicinal chemistry letters.

Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.

S. Gardell, R. Magolda, E. Trybulski, 2009, Journal of medicinal chemistry.

Synthesis of stable thromboxane A2 analogs: pinane thromboxane A2 (PTA2) and carbocyclic thromboxane A2 (CTA2).

K. Nicolaou, R. Magolda, 1982, Methods in enzymology.

6,9-Pyridazaprostacyclin and derivatives: the first "aromatic" prostacyclins

K. Nicolaou, R. Magolda, W. E. Barnette, 1979 .

Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides: part II.

R. Bhat, P. Bodine, G. Krishnamurthy, 2010, Bioorganic & medicinal chemistry.

Preclinical characterization of WAY‐211612: a dual 5‐HT uptake inhibitor and 5‐HT1A receptor antagonist and potential novel antidepressant

R. Magolda, J. Malberg, S. Rosenzweig-Lipson, 2009, British journal of pharmacology.

Discovery of potent and selective PKC-theta inhibitors.

Mohammed A Kashem, C. Homon, J. Woska, 2007, Bioorganic & medicinal chemistry letters.

Terphenyl cyclooxygenase-2 (COX-2) inhibitors: optimization of the central ring and o-biphenyl analogs.

R. Copeland, R. Magolda, J. Trzăskos, 1999, Bioorganic & medicinal chemistry letters.

Prodrugs of perzinfotel with improved oral bioavailability.

B. Harrison, M. Pangalos, R. Magolda, 2009, Journal of medicinal chemistry.

Evolution of the Thienopyridine Class of Inhibitors of IκB Kinase-β: Part I: Hit-to-Lead Strategies

C. Homon, C. Cywin, Jiang-Ping Wu, 2006 .

SIMPLE EFFICIENT SYNTHESIS OF PROSTACYCLIN (PGI2)

G. Gasic, K. Nicolaou, R. Magolda, 1978 .

6,9-THIAPROSTACYCLIN. A STABLE AND BIOLOGICALLY POTENT ANALOG OF PROSTACYCLIN (PGI2)

G. Gasic, K. Nicolaou, R. Magolda, 1978 .

A NEW EFFICIENT AND VERSATILE SYNTHESIS OF ALKYL PHOSPHORYLCHOLINES

R. Magolda, P. Johnson, 1985 .

A new efficient and versatile synthesis of alkyl prosphorylcholines

R. Magolda, Paul R. Johnson, 1985 .

Inhibition of MAP kinase kinase (MEK) results in an anti-inflammatory response in vivo.

E. Manos, B. Jaffee, M. Favata, 2000, Biochemical and biophysical research communications.