C. Decicco

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The Changing Face of Innovation in Drug Discovery

Litao Zhang, C. Decicco, 2014 .

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 .

Identification of a selectivity determinant for inhibition of tumor necrosis factor-alpha converting enzyme by comparative modeling.

David J Nelson, D. J. Nelson, Zelda R Wasserman, 2003, Chemistry & biology.

Role of P-Glycoprotein and the Intestine in the Excretion of DPC 333 [(2R)-2-{(3R)-3-Amino-3-[4-(2-methylquinolin-4-ylmethoxy)phenyl]-2-oxopyrrolidin-1-yl}-N-hydroxy-4-methylpentanamide] in Rodents

T. Maduskuie, C. Garner, C. Decicco, 2008, Drug Metabolism and Disposition.

Constituents of Michelia Rajaniana. Two new germacranolide amides.

N. Ruangrungsi, K. Likhitwitayawuid, C. Decicco, 1988, Journal of natural products.

Pharmacokinetics and Pharmacodynamics of DPC 333 ((2R)-2-((3R)-3-Amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)), a Potent and Selective Inhibitor of Tumor Necrosis Factor α-Converting Enzyme in Rodents, Dogs, Chimpanzees, and Humans

J. Trzăskos, T. Maduskuie, C. Garner, 2007, Drug Metabolism and Disposition.

A molecular modeling analysis of novel non-hydroxamate inhibitors of TACE.

Andrew Tebben, Zelda R Wasserman, A. Tebben, 2007, Bioorganic & medicinal chemistry letters.

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.

Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme.

M. Covington, C. Decicco, J. Duan, 2005, Bioorganic & medicinal chemistry letters.

Design and synthesis of bicyclic pyrimidinone-based HCV NS3 protease inhibitors.

B. Douty, C. Decicco, Peter W Glunz, 2003, Bioorganic & medicinal chemistry letters.

Design and synthesis of bicyclic pyrimidinone-based HCV NS3 protease inhibitors.

B. Douty, C. Decicco, P. Glunz, 2003, Bioorganic & medicinal chemistry letters.

N-in-1 dosing pharmacokinetics in drug discovery: experience, theoretical and practical considerations.

P. Lam, K. He, T. Olah, 2008, Journal of pharmaceutical sciences.

Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.

S. Sheriff, D. Seiffert, J. Bozarth, 2017, Journal of medicinal chemistry.

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.

Generation and Characterization of Aggrecanase

J. Trzăskos, C. Decicco, M. Tortorella, 1999, The Journal of Biological Chemistry.

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.

Potent P1' biphenylmethyl substituted aggrecanase inhibitors.

M. Covington, C. Decicco, R. Wexler, 2002, Bioorganic & medicinal chemistry letters.

Macrocyclic amino carboxylates as selective MMP-8 inhibitors.

W. DeGrado, K. D. Hardman, R. Copeland, 1998, Journal of medicinal chemistry.

Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.

G. Trainor, M. Covington, C. Decicco, 2005, Journal of medicinal chemistry.

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.

A. Good, J. Macor, J. Marcinkeviciene, 2011, Bioorganic & medicinal chemistry letters.

Biosynthesis of 2-(2′-methylthio)ethylmalate in Brassica carinata

C. Chapple, B. Ellis, C. Decicco, 1988 .

CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.

I. Kariv, K. Vaddi, M. Covington, 2007, Bioorganic & medicinal chemistry letters.

Alkylsulfone-containing trisubstituted cyclohexanes as potent and bioavailable chemokine receptor 2 (CCR2) antagonists.

Michael G. Yang, J. Barrish, S. Mandlekar, 2014, Bioorganic & medicinal chemistry letters.

Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

J. Barrish, P. Scherle, M. Cvijic, 2012, Bioorganic & medicinal chemistry letters.

Novel sulfone-containing di- and trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.

P. Scherle, A. Tebben, Gengjie Yang, 2009, Bioorganic & medicinal chemistry letters.

Discovery of trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.

P. Scherle, Gengjie Yang, C. Decicco, 2009, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists.

D. J. Nelson, P. Scherle, Gengjie Yang, 2008, Bioorganic & medicinal chemistry letters.

Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists.

D. J. Nelson, S. Mandlekar, P. Scherle, 2008, Journal of medicinal chemistry.

Mutagenesis and mechanism-based inhibition of Streptococcus pyogenes Glu-tRNAGln amidotransferase implicate a serine-based glutaminase site.

D. J. Nelson, R. Copeland, K. Horiuchi, 2002, Biochemistry.

A new synthesis of cytoxazone and its diastereomers provides key initial SAR information.

P. Scherle, C. Decicco, P. Carter, 2003, Bioorganic & medicinal chemistry letters.

Cytokine-induced cartilage proteoglycan degradation is mediated by aggrecanase.

B. Caterson, C. Hughes, C. Decicco, 1998, Osteoarthritis and cartilage.

CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.

G. Trainor, M. Covington, C. Decicco, 2002, Bioorganic & medicinal chemistry letters.

Macrocyclic hydroxamate inhibitors of matrix metalloproteinases and TNF-α production

K. D. Hardman, R. Copeland, B. Jaffee, 1999 .

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

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

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.

Potent matrix metalloproteinase inhibitors: Amino-carboxylate compounds containing modifications of the P1 residue

W. DeGrado, R. Copeland, C. Decicco, 1996 .

Glutamyl-γ-boronate inhibitors of bacterial Glu-tRNAGln amidotransferase

D. J. Nelson, R. Copeland, K. Horiuchi, 2001 .

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.

Inhibition of tumor necrosis factor-alpha-converting enzyme by a selective antagonist protects brain from focal ischemic injury in rats.

G. Feuerstein, R. Taub, C. Decicco, 2004, Molecular pharmacology.

Evolution of a matrix metalloproteinase assay to assess inhibitor potency and selectivity

R. Copeland, J. Trzăskos, C. Decicco, 1995 .

N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists.

J. Trzăskos, C. Decicco, P. Carter, 2005, Bioorganic & medicinal chemistry letters.

Design and synthesis of cyclic inhibitors of matrix metalloproteinases and TNF-alpha production.

D. J. Nelson, W. DeGrado, K. D. Hardman, 1998, Journal of medicinal chemistry.

Amide surrogates of matrix metalloproteinase inhibitors : Urea and sulfonamide mimics

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

2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity.

G. Trainor, M. Covington, C. Decicco, 2006, Bioorganic & medicinal chemistry letters.

Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.

G. Trainor, M. Covington, C. Decicco, 2004, Bioorganic & medicinal chemistry letters.

Cleavage of Native Cartilage Aggrecan by Neutrophil Collagenase (MMP-8) Is Distinct from Endogenous Cleavage by Aggrecanase*

C. Decicco, M. Tortorella, E. Arner, 1997, The Journal of Biological Chemistry.

Structural elucidation and synthesis of new components isolated from piper sarmentosum piperaceae

N. Ruangrungsi, K. Likhitwitayawuid, C. Decicco, 1987 .

Probing the P3′ pocket of stromelysin with piperazic acid analogs

D. J. Nelson, K. D. Hardman, R. Copeland, 1995 .

Asymmetric induction in mixed [2 + 2] photoadditions. Effect of solvent, alkene concentration and temperature

C. Decicco, Moses Lee, G. L. Lange, 1987 .

Asymmetric Synthesis of 2,3-Disubstituted Succinates via Chiral Oxazolidinone Controlled Displacement of .alpha.-Trifluoromethanesulfonate Substituted Esters

D. J. Nelson, C. Decicco, R. L. Corbett, 1995 .

Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists.

P. Scherle, J. Trzăskos, A. Tebben, 2003, Bioorganic & medicinal chemistry letters.

Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Andrew Tebben, A. Tebben, C. Decicco, 2007, Bioorganic & medicinal chemistry letters.

Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Soong-Hoon Kim, W. Pitts, M. Covington, 2007, Bioorganic & medicinal chemistry letters.

Intramolecular O-arylation of phenols with phenylboronic acids: application to the synthesis of macrocyclic metalloproteinase inhibitors.

C. Decicco, D. Evans, Yingfeng Song, 2001, Organic letters.

Design and synthesis of 6-amino-5-oxo-1,2,3,5-tetrahydro-3-indolizinecarboxylic acids as β-sheet peptidomimetics

C. Decicco, Aaron C. Schmitt, Xiaojun Zhang, 2002 .

Highly enantioselective and diastereoselective synthesis of β-amino acid esters and β-lactams from achiral esters and imines

E. Corey, C. Decicco, R. Newbold, 1991 .

Photochemically enhanced binding of small molecules to the tumor necrosis factor receptor-1 inhibits the binding of TNF-α

D. Underwood, P. Domaille, K. Ramnarayan, 2001, Proceedings of the National Academy of Sciences of the United States of America.

gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Michael G. Yang, J. Barrish, S. Mandlekar, 2010, Bioorganic & medicinal chemistry letters.

α,β-Cyclic-β-benzamido hydroxamic acids: Novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-α converting enzyme (TACE)

David D. Christ, K. Vaddi, M. Covington, 2008 .

Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.

Zelda R Wasserman, J. Trzăskos, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

Conversion of potent MMP inhibitors into selective TACE inhibitors.

Bryan W King, B. W. King, M. Covington, 2006, Bioorganic & medicinal chemistry letters.

Asymmetric induction in mixed photoadditions: Employing α,β-unsaturated homochiral ketals

C. Decicco, G. L. Lange, G. Lange, 1988 .

Heteroaryl-fused 2-phenylisothiazolone inhibitors of cartilage breakdown.

M. Abelman, S. Wright, J. Petraitis, 1994, Journal of medicinal chemistry.

A concise synthesis of silanediol-based transition-state isostere inhibitors of proteases.

A. Combs, C. Decicco, M. Organ, 2002, Organic letters.

Glycine α-Ketoamides as HCV NS3 Protease Inhibitors

C. Decicco, W. Han, Z. Wasserman, 2003 .

Asymmetric induction in simple [2 + 2] photoadditions

C. Decicco, G. L. Lange, S. Tan, 1985 .

Asymmetric synthesis of trans-2,3-piperidinedicarboxylic acid and trans-3,4-piperidinedicarboxylic acid derivatives.

C. Decicco, C. Xue, J. Roderick, 2002, The Journal of organic chemistry.

ASYMMETRIC AMINO ACID SYNTHESIS : MITSUNOBU REACTION ON CHIRAL CYANOHYDRINS

C. Decicco, P. Grover, 1997 .

Chirality as a probe in .beta.-keto ester tautomerism

C. Decicco, Ronald N. Buckle, 1992 .

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

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

Asymmetric Induction in Mixed (2 + 2) Photoadditions. Effect of Solvent, Alkene Concentration and Temperature.

C. Decicco, Moses Lee, G. L. Lange, 1987 .

Capped diaminopropionamide-glycine dipeptides are inhibitors of CC chemokine receptor 2 (CCR2).

P. Scherle, A. Tebben, Gengjie Yang, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors.

Xiaohua He, John Roderick, J. Trzăskos, 2004, Bioorganic & medicinal chemistry letters.

Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

John Roderick, Xiao-tao Chen, M. Covington, 2007, Bioorganic & medicinal chemistry letters.

P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease.

C. Decicco, E. Priestley, I. De Lucca, 2002, Bioorganic & medicinal chemistry letters.

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.

A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.

J. Trzăskos, Xiao-tao Chen, K. Vaddi, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and structure–activity relationship of a novel, achiral series of TNF-α converting enzyme inhibitors

J. Trzăskos, T. Maduskuie, B. W. King, 2004 .

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.

Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.

G. Trainor, M. Covington, C. Decicco, 2004, Bioorganic & medicinal chemistry letters.

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.

Slow-binding inhibition of gamma-glutamyl transpeptidase by gamma-boroGlu.

B. Thomas, R. Stein, C. Decicco, 2001, Biochemistry.

From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.

I. Kariv, S. Mandlekar, A. Tebben, 2008, Bioorganic & medicinal chemistry letters.

Aggrecan Protects Cartilage Collagen from Proteolytic Cleavage*

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

Therapeutic potential and strategies for inhibiting tumor necrosis factor-alpha.

C. Decicco, R. Newton, 1999, Journal of medicinal chemistry.

Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists.

G. Trainor, M. Covington, C. Decicco, 2002, Journal of medicinal chemistry.

The synthesis of pyrimidineisothiazolones. The effect of temperature on the addition of aryl amines to functionalized pyrimidines

C. Decicco, D. Nelson, 1993 .

Design and synthesis of potent, non-peptide inhibitors of HCV NS3 protease.

C. Decicco, Z. Wasserman, Carl P Decicco, 2003, Bioorganic & medicinal chemistry letters.

Synthesis of Biologically Active Piperidine Metabolites of Clopidogrel: Determination of Structure and Analyte Development.

P. Lam, W. Humphreys, A. Mathur, 2015, The Journal of organic chemistry.

Effect of DPC 333 [(2R)-2-{(3R)-3-Amino-3-[4-(2-methylquinolin-4-ylmethoxy)phenyl]-2-oxopyrrolidin-1-yl}-N-hydroxy-4-methylpentanamide], a Human Tumor Necrosis Factor α-Converting Enzyme Inhibitor, on the Disposition of Methotrexate: A Transporter-Based Drug-Drug Interaction Case Study

K. Brouwer, T. Maduskuie, C. Garner, 2007, Drug Metabolism and Disposition.

EFFECT OF DPC 333, A HUMAN TUMOR NECROSIS FACTOR α CONVERTING ENZYME INHIBITOR, ON THE DISPOSITION OF METHOTREXATE: A TRANSPORTER BASED DRUG-DRUG INTERACTION CASE STUDY

K. Brouwer, T. Maduskuie, C. Garner, 2007 .

Inhibition of Tumor Necrosis Factor-α-Converting Enzyme by a Selective Antagonist Protects Brain from Focal Ischemic Injury in Rats

Lin Xu, G. Feuerstein, R. Taub, 2004 .

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

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

Estimating KI values for tight binding inhibitors from dose-response plots

Robert A. Copeland, R. Copeland, C. Decicco, 1995 .

Ring expansions of [2 + 2] photoadducts. Potential applications in the synthesis of triquinane and taxane skeletons

C. Decicco, J. Willson, G. Lange, 1989 .

Sultam hydroxamates as novel matrix metalloproteinase inhibitors.

K. D. Hardman, J. Trzăskos, M. Covington, 2004, Journal of medicinal chemistry.

α-Ketoamides, α-ketoesters and α-diketones as HCV NS3 protease inhibitors

C. Decicco, W. Han, Zilun Hu, 2000 .

Potent carboxylate inhibitors of stromelysin containing P2′ piperazic acids and P1′ biaryl moeities

K. D. Hardman, R. Copeland, C. Decicco, 1997 .

Biology of TACE inhibition

K. Vaddi, M. Covington, P. Haley, 2001, Annals of the rheumatic diseases.

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 and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor.

J. Macor, C. Albright, R. Olson, 2010, ACS medicinal chemistry letters.

Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe

M. Favata, J. Trzăskos, A. Tebben, 2007, Proceedings of the National Academy of Sciences.

Correction to "Synthesis of Biologically Active Piperidine Metabolites of Clopidogrel: Determination of Structure and Analyte Development".

P. Lam, W. Humphreys, A. Mathur, 2015, Journal of Organic 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.

1-Aminocyclopropaneboronic acid: synthesis and incorporation into an inhibitor of hepatitis C virus NS3 protease.

C. Decicco, E. Priestley, 2000, Organic letters.

The fate of pro-TNF-alpha following inhibition of metalloprotease-dependent processing to soluble TNF-alpha in human monocytes.

M. Covington, C. Decicco, R. Newton, 1997, Journal of immunology.

Pharmacologic inhibition of BAF chromatin remodeling complexes as a therapeutic approach to transcription factor-dependent cancers

GiNell Elliott, Lan Xu, S. Topal, 2023, bioRxiv.