Page last updated: 2024-08-21

pyrazines and cgs 27023a

pyrazines has been researched along with cgs 27023a in 58 studies

Research

Studies (58)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's14 (24.14)18.2507
2000's39 (67.24)29.6817
2010's5 (8.62)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Blancuzzi, V; Ganu, VS; Goldberg, RL; Ludewig, R; MacPherson, LJ; O'Byrne, EM; Parker, DT; Roberts, ED; Singh, HN; Wilson, D1
Doughty, J; Ganu, V; Goldberg, RL; O'Byrne, E; Spirito, S1
Pratta, MA1
Bayburt, EK; Blancuzzi, V; Capparelli, MP; Carroll, BJ; Doughty, JR; Fryer, L; Ganu, V; Goldberg, RL; Goldstein, R; Hu, S; Justice, MR; MacPherson, LJ; Melton, RA; O'Byrne, EM; Parker, DT; Spirito, S; Wilson, D; Zhu, L1
Blancuzzi, V; Doughty, JR; Goldberg, RL; O'Byrne, E; Singh, HN; Spirito, S1
Gonnella, NC; Li, YC; Paris, CG; Zhang, X1
Epps, DE; Laborde, AL; Petzold, GL; Poorman, RA; Stuchly, CW; Van Drie, JH1
Albright, JD; DiJoseph, JF; Killar, LM; Levin, JI; Roth, CE; Sharr, MA; Skotnicki, JS; Sung, A; Walter, T1
Chanda, PK; Chen, JM; Cosmi, S; Edris, W; Moy, FJ; Powers, R; Skotnicki, JS; Wilhelm, J1
Caplan, SL; Chou, M; Jeng, AY; Jeune, M; Prescott, MF; Sawyer, WK; Von Linden-Reed, J1
Ganu, V; Melton, R; Roberts, D; Wang, W1
Hande, KR; Nelson, AR; Rothenberg, ML1
Caldarelli, M; Habermann, J; Ley, SV1
Choi, L; Eskens, FA; Harris, AL; Levitt, NC; Mather, R; Sparreboom, A; Verweij, J1
Chiba, T; Ko, K; Konda, Y; Nakajima, M; Takahashi, R; Yazumi, S; Yoshikawa, K1
Brady, CS; FitzGerald, MX; Mackarel, AJ; O'Connor, CM; Russell, KJ1
Chanda, PK; Chen, JM; Cosmi, S; Edris, W; Levin, JI; Moy, FJ; Powers, R1
Hwang, JJ; Ip, MM; Lee, PP; Murphy, G1
Choy, M; Dias, S; Hattori, K; Heissig, B; Lane, WJ; Moore, MA; Rabbany, SY; Rafii, S; Wood, J1
Eckhardt, SG; Hidalgo, M1
Hwang, JJ; Ip, MM; Lee, PP; Mead, L1
Choi, L; Denis, LJ; Eskens, FA; Foekens, JA; Harris, AL; Levitt, NC; Nakajima, M; O'Byrne, KJ; Owen, SJ; Propper, DJ; Steward, WP; Talbot, DC; Verweij, J; Wilner, S; Wood, JM1
Bauer, MM; Dollinger, H; Jung, B; Nar, H; Werle, K1
Albright, JD; Chen, JM; Cowling, R; Delos Santos, E; DiJoseph, JF; Jin, G; Killar, LM; Levin, JI; Nelson, FC; Roth, CE; Sharr, MA; Skotnicki, JS; Sung, A1
Bin Sun, H; Fei, X; Hutchins, GD; Lee Stone, K; Liu, X; Martinez, TD; Miller, KD; Mock, BH; Sledge, GW; Wang, JQ; Zheng, QH1
Antolín, M; Guarner, F; Malagelada, JR; Medina, C; Radomski, A; Radomski, MW; Salas, A; Videla, S; Vilaseca, J1
Hirayama, R; Inoue, Y; Ishibushi, E; Ito, Y; Kiyoi, T; Kondo, H; Kumihara, H; Miyasaka, T; Nakajima, F; Ohmoto, H; Sawa, M; Yamamoto, M; Yamamoto, T; Yoshiizumi, K; Yoshino, K1
Corbett, RL; Covington, MB; Decicco, CP; Duan, JJ; He, X; Liu, RQ; Magolda, RL; Newton, RC; Roderick, J; Trzaskos, JM; Wexler, RR; Xue, CB1
Kawai, N; Kawanishi, M; Nagao, S1
Breyholz, HJ; Guilbert, B; Kopka, K; Law, MP; Levkau, B; Riemann, B; Schäfers, M; Schober, O; Schröer, S; Trub, M; Wagner, S1
DiMicco, MA; Grodzinsky, AJ; Kim, YJ; Kumar, S; Lark, MW; Patwari, P; Pratta, MA; Siparsky, PN1
Majumdar, TK; Tse, FL; Vedananda, S1
Breyholz, HJ; Kopka, K; Law, MP; Levkau, B; Riemann, B; Schäfers, KP; Schäfers, M; Schober, O; Wagner, S1
Hattori, K; Nakajima, M; Nakashima, E; Oku, N; Tamura, M; Tsukada, H; Unno, K; Yonezawa, S1
Blackey, R; Cassidy, J; Choi, L; Devlin, M; Eatock, M; Johnson, J; Morrison, R; Owen, S; Twelves, C1
Li, MY; Matsumoto, K; Mizuno, S; Nakamura, T1
Askew, C; Cosgrove, D; Gratton, MA; Meehan, DT; Rao, VH1
Matono, K; Mizobe, T; Nagase, H; Nakajima, M; Ogata, Y; Sasatomi, T; Shirouzu, K1
Adachi, E; Akutsu, N; Amano, S; Kadoya, K; Matsunaga, Y; Nishiyama, T; Ogura, Y1
Díaz-Gonzalez, F; Farre, E; Medina, C; Paz, MC; Quintero, E; Radomski, MW; Salas, A; Santana, A1
Fujita, M; Harada, E; Ikegame, S; Inoshima, I; Nakanishi, Y; Ouchi, H; Ye, Q1
Howes, JM; Laing, GD; Theakston, RD1
Amano, S; Ehama, R; Matsunaga, Y; Nishiyama, T; Ogura, Y; Tagami, H1
Breyholz, HJ; Kopka, K; Levkau, B; Schäfers, M; Schober, O; Wagner, S1
Breyholz, HJ; Faust, A; Haufe, G; Höltke, C; Kopka, K; Law, MP; Levkau, B; Schäfers, M; Schober, O; Schröer, S; Wagner, S1
Fujita, M; Harada, E; Ikegame, S; Inoshima, I; Kuwano, K; Nakanishi, Y; Ouchi, H; Ye, Q1
Burke, SL; Huang, Z; Karnachi, P; Lagu, B; Murray, WV; Rhodes, KJ; Scannevin, RH; Wang, B; Wilson, LJ; Yang, SM1
Burke, SL; Karnachi, P; Lagu, B; Murray, WV; Rhodes, KJ; Scannevin, RH; Wang, B; Wilson, LJ; Yang, SM1
Kasaoka, T; Nakajima, M; Nishiyama, H; Okada, M1
Breyholz, HJ; Faust, A; Höltke, C; Kopka, K; Schäfers, M; Schober, O; Wagner, S1
Agrawal, A; Cohen, S; Jacobsen, J; Romero-Perez, D; Thomas, R; Villarreal, F; Yan, Y1
Bremer, C; Breyholz, HJ; Faust, A; Heindel, W; Höltke, C; Kopka, K; Schäfers, M; Schober, O; Wagner, S; Waldeck, J; Waschkau, B1
Agback, T; Isaksson, J; Kovacs, H1
Baldock, PA; Kostenuik, PJ; Little, DG; McDonald, MM; Mikulec, K; Morse, A; Peacock, L1
Fisher, GJ; Hammerberg, C; He, T; Li, Y; Quan, T; Voorhees, JJ; Xia, W1
Behrends, M; Haufe, G; Kopka, K; Kumbhar, S; Schäfers, M; Schober, O; Wagner, S; Waller, M1
Cook, H; Gillen, K; Large, JM; Love, EA; Matthews, D; Merritt, A; Patel, S; Sattikar, A1

Reviews

1 review(s) available for pyrazines and cgs 27023a

ArticleYear
Development of matrix metalloproteinase inhibitors in cancer therapy.
    Journal of the National Cancer Institute, 2001, Feb-07, Volume: 93, Issue:3

    Topics: Animals; Antibiotics, Antineoplastic; Antineoplastic Agents; Biphenyl Compounds; Clinical Trials as Topic; Drugs, Investigational; Enzyme Inhibitors; Humans; Hydroxamic Acids; Imidazoles; Matrix Metalloproteinase Inhibitors; Neoplasms; Organic Chemicals; Phenylalanine; Phenylbutyrates; Protease Inhibitors; Pyrazines; Sulfonamides; Tetracycline; Tetracyclines; Thiophenes

2001

Trials

3 trial(s) available for pyrazines and cgs 27023a

ArticleYear
Effect of food on the pharmacokinetics of oral MMI270B (CGS 27023A), a novel matrix metalloproteinase inhibitor.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2000, Volume: 6, Issue:2

    Topics: Administration, Oral; Area Under Curve; Dose-Response Relationship, Drug; Eating; Fasting; Humans; Hydroxamic Acids; Metalloendopeptidases; Neoplasms; Postprandial Period; Protease Inhibitors; Pyrazines; Sulfonamides

2000
Phase I and pharmacological study of the oral matrix metalloproteinase inhibitor, MMI270 (CGS27023A), in patients with advanced solid cancer.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2001, Volume: 7, Issue:7

    Topics: Administration, Oral; Adult; Aged; Area Under Curve; Dose-Response Relationship, Drug; Exanthema; Female; Humans; Hydroxamic Acids; Male; Metabolic Clearance Rate; Metalloendopeptidases; Middle Aged; Musculoskeletal Diseases; Nausea; Neoplasms; Protease Inhibitors; Pyrazines; Sulfonamides; Treatment Outcome

2001
A dose-finding and pharmacokinetic study of the matrix metalloproteinase inhibitor MMI270 (previously termed CGS27023A) with 5-FU and folinic acid.
    Cancer chemotherapy and pharmacology, 2005, Volume: 55, Issue:1

    Topics: Administration, Oral; Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Colonic Neoplasms; Drug Interactions; Female; Fluorouracil; Humans; Hydroxamic Acids; Leucovorin; Male; Metalloendopeptidases; Middle Aged; Protease Inhibitors; Pyrazines; Rectal Neoplasms; Sulfonamides

2005

Other Studies

54 other study(ies) available for pyrazines and cgs 27023a

ArticleYear
Oral administration of a matrix metalloproteinase inhibitor, CGS 27023A, protects the cartilage proteoglycan matrix in a partial meniscectomy model of osteoarthritis in rabbits.
    Inflammation research : official journal of the European Histamine Research Society ... [et al.], 1995, Volume: 44 Suppl 2

    Topics: Animals; Cartilage, Articular; Hindlimb; Hydroxamic Acids; Joints; Male; Metalloendopeptidases; Osteoarthritis; Protease Inhibitors; Proteoglycans; Pyrazines; Rabbits; Sulfonamides

1995
Metalloprotease inhibitors halt collagen breakdown in IL-1 induced bovine nasal cartilage cultures.
    Inflammation research : official journal of the European Histamine Research Society ... [et al.], 1995, Volume: 44 Suppl 2

    Topics: Animals; Cartilage; Cattle; Collagen; Hydroxamic Acids; Interleukin-1; Metalloendopeptidases; Nasal Mucosa; Nose; Organ Culture Techniques; Protease Inhibitors; Proteoglycans; Pyrazines; Sulfonamides

1995
Biological evaluation of matrix metalloproteinase inhibitors, 18 May 1995, New York.
    Inflammation research : official journal of the European Histamine Research Society ... [et al.], 1995, Volume: 44, Issue:11

    Topics: Animals; Humans; Hydroxamic Acids; Metalloendopeptidases; Osteoarthritis; Protease Inhibitors; Proteoglycans; Pyrazines; Sulfonamides

1995
Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits.
    Journal of medicinal chemistry, 1997, Aug-01, Volume: 40, Issue:16

    Topics: Administration, Oral; Animals; Binding Sites; Cartilage; Chromatography, High Pressure Liquid; Enzyme-Linked Immunosorbent Assay; Humans; Hydroxamic Acids; In Vitro Techniques; Kinetics; Matrix Metalloproteinase Inhibitors; Models, Chemical; Protease Inhibitors; Pyrazines; Rabbits; Rats; Recombinant Proteins; Structure-Activity Relationship; Substance P; Sulfonamides

1997
The effect of CGS 27023A on the level of 3B3 (-) epitope in a rabbit meniscectomy model.
    Inflammation research : official journal of the European Histamine Research Society ... [et al.], 1997, Volume: 46 Suppl 2

    Topics: Animals; Enzyme-Linked Immunosorbent Assay; Epitopes; Glucuronates; Glucuronic Acid; Hydroxamic Acids; Kinetics; Knee Joint; Male; Menisci, Tibial; Metalloendopeptidases; Osteoarthritis; Protease Inhibitors; Pyrazines; Rabbits; Sulfonamides

1997
Bioactive conformation of a potent stromelysin inhibitor determined by X-nucleus filtered and multidimensional NMR spectroscopy.
    Bioorganic & medicinal chemistry, 1997, Volume: 5, Issue:12

    Topics: Binding Sites; Collagenases; Computer Simulation; Fibroblasts; Humans; Hydroxamic Acids; Magnetic Resonance Spectroscopy; Matrix Metalloproteinase 3; Matrix Metalloproteinase Inhibitors; Models, Molecular; Protease Inhibitors; Protein Binding; Protein Conformation; Pyrazines; Sulfonamides

1997
The constituent tryptophans and bisANS as fluorescent probes of the active site and of a secondary binding site of stromelysin-1 (MMP-3).
    Journal of protein chemistry, 1998, Volume: 17, Issue:7

    Topics: Acrylamides; Anilino Naphthalenesulfonates; Binding Sites; Catalytic Domain; Fluorescence Polarization; Fluorescent Dyes; Hydroxamic Acids; Matrix Metalloproteinase 3; Matrix Metalloproteinase Inhibitors; Models, Chemical; Phenylalanine; Protease Inhibitors; Protein Binding; Pyrazines; Spectrometry, Fluorescence; Sulfonamides; Thiophenes; Tryptophan

1998
The synthesis and biological activity of a novel series of diazepine MMP inhibitors.
    Bioorganic & medicinal chemistry letters, 1998, Oct-06, Volume: 8, Issue:19

    Topics: Animals; Antineoplastic Agents; Azepines; Enzyme Inhibitors; Hydroxamic Acids; Matrix Metalloproteinase 1; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Mice; Organic Chemicals; Protease Inhibitors; Pyrazines; Structure-Activity Relationship; Sulfonamides

1998
NMR solution structure of the catalytic fragment of human fibroblast collagenase complexed with a sulfonamide derivative of a hydroxamic acid compound.
    Biochemistry, 1999, Jun-01, Volume: 38, Issue:22

    Topics: Catalysis; Collagenases; Computer Simulation; Crystallography, X-Ray; Fibroblasts; Humans; Hydroxamic Acids; Macromolecular Substances; Matrix Metalloproteinase 1; Matrix Metalloproteinase 3; Matrix Metalloproteinase 8; Matrix Metalloproteinase Inhibitors; Models, Molecular; Nuclear Magnetic Resonance, Biomolecular; Peptide Fragments; Protease Inhibitors; Protein Conformation; Pyrazines; Solutions; Sulfonamides

1999
Effect of matrix metalloproteinase inhibition on progression of atherosclerosis and aneurysm in LDL receptor-deficient mice overexpressing MMP-3, MMP-12, and MMP-13 and on restenosis in rats after balloon injury.
    Annals of the New York Academy of Sciences, 1999, Jun-30, Volume: 878

    Topics: Animals; Aorta, Abdominal; Aortic Aneurysm, Abdominal; Arteriosclerosis; Carotid Arteries; Carotid Artery Injuries; Catheterization; Cell Movement; Collagenases; Elastin; Hydroxamic Acids; Male; Matrix Metalloproteinase 12; Matrix Metalloproteinase 13; Matrix Metalloproteinase 3; Metalloendopeptidases; Mice; Mice, Knockout; Protease Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley; Receptors, LDL; Recurrence; Sulfonamides; Transcription, Genetic

1999
Matrix metalloproteinase inhibitor CGS 27023A protects COMP and proteoglycan in the bovine articular cartilage but not the release of their fragments from cartilage after prolonged stimulation in vitro with IL-1 alpha.
    Annals of the New York Academy of Sciences, 1999, Jun-30, Volume: 878

    Topics: Animals; Cartilage Oligomeric Matrix Protein; Cartilage, Articular; Cattle; Extracellular Matrix Proteins; Glycoproteins; Humans; Hydroxamic Acids; Interleukin-1; Kinetics; Matrilin Proteins; Metalloendopeptidases; Organ Culture Techniques; Protease Inhibitors; Proteoglycans; Pyrazines; Recombinant Proteins; Sulfonamides; Time Factors

1999
New drugs on the horizon: matrix metalloproteinase inhibitors.
    Stem cells (Dayton, Ohio), 1999, Volume: 17, Issue:4

    Topics: Antineoplastic Agents; Azepines; Biphenyl Compounds; Humans; Hydroxamic Acids; Metalloendopeptidases; Organic Chemicals; Phenylalanine; Phenylbutyrates; Protease Inhibitors; Pyrazines; Sulfonamides; Thiophenes

1999
Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents.
    Bioorganic & medicinal chemistry letters, 1999, Jul-19, Volume: 9, Issue:14

    Topics: Chemistry, Organic; Chromatography, Liquid; Hydroxamic Acids; Indicators and Reagents; Magnetic Resonance Spectroscopy; Mass Spectrometry; Matrix Metalloproteinase Inhibitors; Metalloendopeptidases; Polymers; Protease Inhibitors; Pyrazines; Sulfonamides

1999
CGS 27023A. CDG 27023A.
    Drugs in R&D, 1999, Volume: 1, Issue:2

    Topics: Animals; Antineoplastic Agents; Antirheumatic Agents; Drugs, Investigational; Humans; Hydroxamic Acids; Metalloendopeptidases; Mice; Neoplasms; Protease Inhibitors; Pyrazines; Rabbits; Rats; Rheumatic Diseases; Sulfonamides

1999
Activation of fibroblast-derived matrix metalloproteinase-2 by colon-cancer cells in non-contact Co-cultures.
    International journal of cancer, 2000, Jul-15, Volume: 87, Issue:2

    Topics: Basement Membrane; Blotting, Northern; Caco-2 Cells; Cell Line; Cell Membrane; Chelating Agents; Coculture Techniques; Colonic Neoplasms; Edetic Acid; Enzyme Activation; Fibroblasts; Gelatin; Humans; Hydroxamic Acids; Matrix Metalloproteinase 2; Matrix Metalloproteinases, Membrane-Associated; Metalloendopeptidases; Protease Inhibitors; Pyrazines; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Sulfonamides; Tissue Inhibitor of Metalloproteinase-2; Tumor Cells, Cultured

2000
Interleukin-8 and leukotriene-B(4), but not formylmethionyl leucylphenylalanine, stimulate CD18-independent migration of neutrophils across human pulmonary endothelial cells in vitro.
    American journal of respiratory cell and molecular biology, 2000, Volume: 23, Issue:2

    Topics: CD11 Antigens; CD18 Antigens; Cell Line; Cell Movement; Chemotactic Factors; Dose-Response Relationship, Drug; Endothelium, Vascular; Glycine; Humans; Hydroxamic Acids; Interleukin-8; L-Selectin; Leukotriene B4; Lung; N-Formylmethionine Leucyl-Phenylalanine; Neutrophils; Permeability; Phenylalanine; Protease Inhibitors; Pyrazines; Sulfonamides; Thiophenes

2000
High-resolution solution structure of the catalytic fragment of human collagenase-3 (MMP-13) complexed with a hydroxamic acid inhibitor.
    Journal of molecular biology, 2000, Sep-22, Volume: 302, Issue:3

    Topics: Amino Acid Sequence; Binding Sites; Catalytic Domain; Collagenases; Crystallography, X-Ray; Humans; Hydroxamic Acids; Inhibitory Concentration 50; Matrix Metalloproteinase 1; Matrix Metalloproteinase 13; Matrix Metalloproteinase Inhibitors; Models, Molecular; Molecular Sequence Data; Nuclear Magnetic Resonance, Biomolecular; Peptide Fragments; Protease Inhibitors; Protein Structure, Secondary; Pyrazines; Sequence Alignment; Sequence Homology, Amino Acid; Solutions; Sulfonamides; Zinc

2000
Functional significance of MMP-9 in tumor necrosis factor-induced proliferation and branching morphogenesis of mammary epithelial cells.
    Endocrinology, 2000, Volume: 141, Issue:10

    Topics: Animals; Antibodies; Cell Division; Cells, Cultured; Enzyme Induction; Epithelial Cells; Female; Hydroxamic Acids; Mammary Glands, Animal; Matrix Metalloproteinase 9; Phenylalanine; Protease Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley; Sulfonamides; Thiophenes; Tumor Necrosis Factor-alpha

2000
Stromal-derived factor 1-induced megakaryocyte migration and platelet production is dependent on matrix metalloproteinases.
    Blood, 2000, Dec-15, Volume: 96, Issue:13

    Topics: Adult; Animals; Blood Platelets; Cells, Cultured; Chemokine CXCL12; Chemokines, CXC; Chemotactic Factors; Chemotaxis; Culture Media, Serum-Free; Enzyme Induction; Extracellular Matrix Proteins; Humans; Hydroxamic Acids; Leukemia, Megakaryoblastic, Acute; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Megakaryocytes; Metalloendopeptidases; Mice; Mice, Inbred BALB C; Protease Inhibitors; Pyrazines; Receptors, CXCR4; Recombinant Fusion Proteins; Sulfonamides; Thrombin; Thrombopoietin; Tissue Inhibitor of Metalloproteinase-1; Transfection; Tumor Cells, Cultured

2000
Functional role of matrix metalloproteinases (MMPs) in mammary epithelial cell development.
    Journal of cellular physiology, 2001, Volume: 188, Issue:1

    Topics: Animals; Cell Size; Cells, Cultured; Culture Media, Conditioned; Culture Media, Serum-Free; Epidermal Growth Factor; Epithelial Cells; Extracellular Matrix; Female; Gelatinases; Humans; Hydroxamic Acids; Immunoblotting; Mammary Glands, Animal; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Mice; Organoids; Peptides; Phenylalanine; Phenylmercury Compounds; Protease Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley; Sulfonamides; Thiophenes; Transforming Growth Factor alpha

2001
Crystal structure of human macrophage elastase (MMP-12) in complex with a hydroxamic acid inhibitor.
    Journal of molecular biology, 2001, Sep-28, Volume: 312, Issue:4

    Topics: Amino Acid Sequence; Binding Sites; Cations, Divalent; Crystallization; Crystallography, X-Ray; Drug Design; Humans; Hydrogen Bonding; Hydroxamic Acids; Macrophages; Matrix Metalloproteinase 12; Metalloendopeptidases; Models, Molecular; Molecular Sequence Data; Protease Inhibitors; Protein Conformation; Pyrazines; Sequence Alignment; Substrate Specificity; Sulfonamides; Zinc

2001
Benzodiazepine inhibitors of the MMPs and TACE.
    Bioorganic & medicinal chemistry letters, 2002, Oct-21, Volume: 12, Issue:20

    Topics: ADAM Proteins; ADAM17 Protein; Benzodiazepines; Cartilage; Hydroxamic Acids; Indicators and Reagents; Matrix Metalloproteinase Inhibitors; Metalloendopeptidases; Protease Inhibitors; Pyrazines; Structure-Activity Relationship; Sulfonamides

2002
Synthesis and preliminary biological evaluation of MMP inhibitor radiotracers [11C]methyl-halo-CGS 27023A analogs, new potential PET breast cancer imaging agents.
    Nuclear medicine and biology, 2002, Volume: 29, Issue:7

    Topics: Animals; Biomarkers, Tumor; Breast Neoplasms; Carbon Radioisotopes; Humans; Hydroxamic Acids; Metalloendopeptidases; Protease Inhibitors; Pyrazines; Radiopharmaceuticals; Sulfonamides; Tomography, Emission-Computed

2002
Increased activity and expression of matrix metalloproteinase-9 in a rat model of distal colitis.
    American journal of physiology. Gastrointestinal and liver physiology, 2003, Volume: 284, Issue:1

    Topics: Animals; Anticoagulants; Colitis, Ulcerative; Colon; Dextran Sulfate; Diarrhea; Disease Models, Animal; Gastrointestinal Hemorrhage; Hydroxamic Acids; Male; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Protease Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley; Sulfonamides

2003
Synthesis and structure-activity relationships of 5,6,7,8-tetrahydropyrido[3,4-b]pyrazine-based hydroxamic acids as HB-EGF shedding inhibitors.
    Bioorganic & medicinal chemistry, 2003, Feb-06, Volume: 11, Issue:3

    Topics: Epidermal Growth Factor; Heparin-binding EGF-like Growth Factor; Humans; Hydroxamic Acids; Intercellular Signaling Peptides and Proteins; Protease Inhibitors; Pyrazines; Stereoisomerism; Structure-Activity Relationship; Sulfonamides; Tumor Cells, Cultured

2003
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.
    Bioorganic & medicinal chemistry letters, 2003, Dec-15, Volume: 13, Issue:24

    Topics: ADAM Proteins; ADAM17 Protein; Drug Design; Enzyme Inhibitors; Hydroxamic Acids; Metalloendopeptidases; Models, Molecular; Molecular Conformation; Protease Inhibitors; Pyrazines; Structure-Activity Relationship; Succinates; Sulfonamides

2003
Treatment of cold injury-induced brain edema with a nonspecific matrix metalloproteinase inhibitor MMI270 in rats.
    Acta neurochirurgica. Supplement, 2003, Volume: 86

    Topics: Animals; Blood-Brain Barrier; Body Water; Brain; Brain Edema; Brain Injuries; Capillary Permeability; Cold Temperature; Enzyme Inhibitors; Hydroxamic Acids; Male; Matrix Metalloproteinase Inhibitors; Parietal Lobe; Pyrazines; Rats; Rats, Sprague-Dawley; Staining and Labeling; Sulfonamides

2003
Synthesis and preliminary biological evaluation of new radioiodinated MMP inhibitors for imaging MMP activity in vivo.
    Nuclear medicine and biology, 2004, Volume: 31, Issue:2

    Topics: Animals; Feasibility Studies; Hydroxamic Acids; Iodine Radioisotopes; Isotope Labeling; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Metabolic Clearance Rate; Mice; Mice, Inbred C57BL; Organ Specificity; Pilot Projects; Pyrazines; Radiopharmaceuticals; Sulfonamides; Tissue Distribution

2004
Mechanisms and kinetics of glycosaminoglycan release following in vitro cartilage injury.
    Arthritis and rheumatism, 2004, Volume: 50, Issue:3

    Topics: Animals; Cartilage, Articular; Cattle; Cell Survival; Dipeptides; Endopeptidases; Glycosaminoglycans; Hydroxamic Acids; In Vitro Techniques; Indenes; Kinetics; Pressure; Protease Inhibitors; Pyrazines; Sulfonamides; Time Factors; Wounds and Injuries

2004
Rapid analysis of MMI270B, an inhibitor of matrix metalloproteases in human plasma by liquid chromatography-tandem mass spectrometry: matrix interference in patient samples.
    Biomedical chromatography : BMC, 2004, Volume: 18, Issue:2

    Topics: Chromatography, Liquid; Humans; Hydroxamic Acids; Mass Spectrometry; Matrix Metalloproteinase Inhibitors; Protease Inhibitors; Pyrazines; Reproducibility of Results; Sensitivity and Specificity; Sulfonamides

2004
Scintigraphic imaging of matrix metalloproteinase activity in the arterial wall in vivo.
    Circulation, 2004, Jun-01, Volume: 109, Issue:21

    Topics: Animals; Apolipoproteins E; Autoradiography; Carotid Artery, Common; Diet, Atherogenic; Feasibility Studies; Hydroxamic Acids; Iodine Radioisotopes; Ligation; Macrophages; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Mice; Mice, Inbred C57BL; Mice, Knockout; Protease Inhibitors; Pyrazines; Radionuclide Imaging; Radiopharmaceuticals; Sulfonamides

2004
In vivo trafficking of endothelial progenitor cells their possible involvement in the tumor neovascularization.
    Life sciences, 2004, Jun-18, Volume: 75, Issue:5

    Topics: Animals; Cell Line, Tumor; Cell Movement; Dose-Response Relationship, Drug; Endothelium, Vascular; Fluorodeoxyglucose F18; Gamma Rays; Hydroxamic Acids; Metalloendopeptidases; Neoplasm Transplantation; Neoplasms, Experimental; Neovascularization, Pathologic; Pyrazines; Rats; Stem Cells; Sulfonamides; Tomography, Emission-Computed

2004
HGF reduces advancing lung fibrosis in mice: a potential role for MMP-dependent myofibroblast apoptosis.
    FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 2005, Volume: 19, Issue:6

    Topics: Actins; Animals; Apoptosis; Bleomycin; Cell Line; Enzyme Inhibitors; Fibroblasts; Fibronectins; Hepatocyte Growth Factor; Humans; Hydroxamic Acids; Lung; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Mice; Mice, Inbred C57BL; Muscle Cells; Proto-Oncogene Proteins c-met; Pulmonary Fibrosis; Pyrazines; Recombinant Proteins; Signal Transduction; Sulfonamides; Tissue Distribution

2005
Matrix metalloproteinase dysregulation in the stria vascularis of mice with Alport syndrome: implications for capillary basement membrane pathology.
    The American journal of pathology, 2005, Volume: 166, Issue:5

    Topics: Animals; Basement Membrane; Capillaries; Computer Systems; Hydroxamic Acids; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Mice; Mice, Knockout; Nephritis, Hereditary; Protease Inhibitors; Pyrazines; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Stria Vascularis; Sulfonamides

2005
Efficacy of the MMP inhibitor MMI270 against lung metastasis following removal of orthotopically transplanted human colon cancer in rat.
    International journal of cancer, 2006, Jan-01, Volume: 118, Issue:1

    Topics: Administration, Oral; Animals; Apoptosis; Chemoprevention; Colonic Neoplasms; Humans; Hydroxamic Acids; Lung Neoplasms; Neoplastic Cells, Circulating; Neovascularization, Pathologic; Pyrazines; Rats; Rats, Nude; Sulfonamides; Survival Analysis; Transplantation, Heterologous

2006
Protective effect of matrix metalloproteinase inhibitors against epidermal basement membrane damage: skin equivalents partially mimic photoageing process.
    The British journal of dermatology, 2005, Volume: 153 Suppl 2

    Topics: Basement Membrane; Cell Adhesion Molecules; Cells, Cultured; Collagen Type IV; Collagen Type VII; Enzyme-Linked Immunosorbent Assay; Epidermis; Humans; Hydroxamic Acids; Kalinin; Male; Matrix Metalloproteinase 1; Matrix Metalloproteinase 2; Matrix Metalloproteinase 3; Matrix Metalloproteinase 9; Microscopy, Electron; Models, Biological; Oligopeptides; Protease Inhibitors; Pyrazines; Skin Aging; Sulfonamides; Tissue Inhibitor of Metalloproteinase-1; Tissue Inhibitor of Metalloproteinase-2; Ultraviolet Rays

2005
Matrix metalloproteinase-9 modulates intestinal injury in rats with transmural colitis.
    Journal of leukocyte biology, 2006, Volume: 79, Issue:5

    Topics: Animals; Colitis; Colon; Disease Models, Animal; Enzyme Activation; Enzyme Inhibitors; Hydroxamic Acids; Inflammation Mediators; Intestinal Mucosa; Male; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Neutrophils; Pyrazines; Rats; Rats, Sprague-Dawley; Sulfonamides; Trinitrobenzenesulfonic Acid; Up-Regulation

2006
Doxycycline attenuated lung injury by its biological effect apart from its antimicrobial function.
    Pulmonary pharmacology & therapeutics, 2007, Volume: 20, Issue:6

    Topics: Animals; Anti-Bacterial Agents; Disease Models, Animal; Doxycycline; Drug Resistance, Bacterial; Hydroxamic Acids; Immunologic Factors; Inflammation; Lipopolysaccharides; Lung; Lung Diseases; Matrix Metalloproteinases; Mice; Mice, Inbred C57BL; Neutrophils; Pulmonary Alveoli; Pyrazines; Streptococcus pneumoniae; Sulfonamides

2007
Neutralization of the haemorrhagic activities of viperine snake venoms and venom metalloproteinases using synthetic peptide inhibitors and chelators.
    Toxicon : official journal of the International Society on Toxinology, 2007, Volume: 49, Issue:5

    Topics: Animals; Biphenyl Compounds; Chelating Agents; Chromatography, Gel; Chromatography, Liquid; Edetic Acid; Egtazic Acid; Ethylenediamines; Evaluation Studies as Topic; Hemorrhage; Hydroxamic Acids; Metalloproteases; Mice; Molecular Structure; Organic Chemicals; Phenylbutyrates; Protein Kinase Inhibitors; Pyrazines; Snake Bites; Statistics, Nonparametric; Sulfonamides; Viper Venoms

2007
Establishment of a mouse skin model of the lichenification in human chronic eczematous dermatitis.
    The British journal of dermatology, 2007, Volume: 156, Issue:5

    Topics: Animals; Disease Models, Animal; Eczema; Epidermis; Glycine; Glycine Agents; Humans; Hydroxamic Acids; Male; Metalloendopeptidases; Mice; Mice, Hairless; Pyrazines; Skin Aging; Sulfonamides

2007
A 18F-radiolabeled analogue of CGS 27023A as a potential agent for assessment of matrix-metalloproteinase activity in vivo.
    The quarterly journal of nuclear medicine and molecular imaging : official publication of the Italian Association of Nuclear Medicine (AIMN) [and] the International Association of Radiopharmacology (IAR), [and] Section of the Society of..., 2007, Volume: 51, Issue:1

    Topics: Drug Delivery Systems; Enzyme Activation; Feasibility Studies; Fluorine Radioisotopes; Hydroxamic Acids; Isotope Labeling; Matrix Metalloproteinases; Pyrazines; Radiopharmaceuticals; Sulfonamides

2007
Novel fluorinated derivatives of the broad-spectrum MMP inhibitors N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](benzyl)- and (3-picolyl)-amino]-3-methyl-butanamide as potential tools for the molecular imaging of activated MMPs with PET.
    Journal of medicinal chemistry, 2007, Nov-15, Volume: 50, Issue:23

    Topics: Animals; Enzyme Activation; Female; Fluorine Radioisotopes; Humans; Hydroxamic Acids; Ligands; Male; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Mice; Mice, Inbred C57BL; Positron-Emission Tomography; Pyrazines; Radiopharmaceuticals; Stereoisomerism; Structure-Activity Relationship; Sulfonamides; Tissue Distribution

2007
The role of collagenases in experimental pulmonary fibrosis.
    Pulmonary pharmacology & therapeutics, 2008, Volume: 21, Issue:2

    Topics: Administration, Oral; Animals; Bleomycin; Bronchoalveolar Lavage Fluid; Collagenases; Gelatin; Hydroxamic Acids; Hydroxyproline; Immunoblotting; Male; Matrix Metalloproteinase Inhibitors; Mice; Mice, Inbred ICR; Protease Inhibitors; Pulmonary Fibrosis; Pyrazines; Sulfonamides

2008
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents.
    Bioorganic & medicinal chemistry letters, 2008, Feb-01, Volume: 18, Issue:3

    Topics: Amino Acids; Animals; Brain Edema; Disease Models, Animal; Drug Design; Gelatinases; Humans; Hydroxamic Acids; Matrix Metalloproteinase Inhibitors; Microsomes, Liver; Middle Cerebral Artery; Molecular Structure; Pyrazines; Rats; Stereoisomerism; Structure-Activity Relationship; Sulfonamides

2008
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 1. Design, synthesis, and lead identification.
    Bioorganic & medicinal chemistry letters, 2008, Feb-01, Volume: 18, Issue:3

    Topics: Animals; Drug Design; Gelatinases; Humans; Hydroxamic Acids; Matrix Metalloproteinase Inhibitors; Microsomes, Liver; Molecular Structure; Pyrazines; Rats; Structure-Activity Relationship; Sulfonamides

2008
Matrix metalloproteinase inhibitor, MMI270 (CGS27023A) inhibited hematogenic metastasis of B16 melanoma cells in both experimental and spontaneous metastasis models.
    Clinical & experimental metastasis, 2008, Volume: 25, Issue:7

    Topics: Animals; Hydroxamic Acids; Lung Neoplasms; Male; Matrix Metalloproteinase Inhibitors; Melanoma, Experimental; Mice; Neoplasm Metastasis; Protease Inhibitors; Pyrazines; Sulfonamides

2008
A new 18F-labelled derivative of the MMP inhibitor CGS 27023A for PET: radiosynthesis and initial small-animal PET studies.
    Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine, 2009, Volume: 67, Issue:4

    Topics: Animals; Fluorine Radioisotopes; Hydroxamic Acids; Matrix Metalloproteinase Inhibitors; Mice; Mice, Inbred C57BL; Positron-Emission Tomography; Protease Inhibitors; Pyrazines; Sulfonamides

2009
Effects of novel semiselective matrix metalloproteinase inhibitors on ex vivo cardiac structure-function.
    Journal of cardiovascular pharmacology, 2009, Volume: 53, Issue:6

    Topics: Animals; Coronary Circulation; Hydroxamic Acids; Male; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Myocardial Contraction; Myocardial Stunning; Oligopeptides; Pyrazines; Pyridones; Pyrones; Rats; Rats, Sprague-Dawley; Reperfusion Injury; Sulfonamides

2009
Synthesis and evaluation of a novel hydroxamate based fluorescent photoprobe for imaging of matrix metalloproteinases.
    Bioconjugate chemistry, 2009, May-20, Volume: 20, Issue:5

    Topics: Carbocyanines; Cell Line, Tumor; Enzyme Inhibitors; Fluorescent Dyes; Humans; Hydroxamic Acids; Ligands; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Molecular Imaging; Polyethylene Glycols; Protein Biosynthesis; Pyrazines; Sulfonamides; Transcription, Genetic

2009
Probing water-protein contacts in a MMP-12/CGS27023A complex by nuclear magnetic resonance spectroscopy.
    Journal of biomolecular NMR, 2012, Volume: 53, Issue:2

    Topics: Humans; Hydroxamic Acids; Matrix Metalloproteinase 12; Matrix Metalloproteinase Inhibitors; Nitrogen Isotopes; Nuclear Magnetic Resonance, Biomolecular; Protease Inhibitors; Protein Conformation; Pyrazines; Sulfonamides; Water

2012
Matrix metalloproteinase-driven endochondral fracture union proceeds independently of osteoclast activity.
    Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research, 2013, Volume: 28, Issue:7

    Topics: Animals; Bone Density Conservation Agents; Clodronic Acid; Collagenases; Diphosphonates; Femoral Fractures; Fracture Healing; Humans; Hydroxamic Acids; Imidazoles; Male; Matrix Metalloproteinase Inhibitors; Osteoclasts; Osteoprotegerin; Pyrazines; Rats; Rats, Wistar; Recombinant Proteins; Sulfonamides; Time Factors; Zoledronic Acid

2013
Expression of catalytically active matrix metalloproteinase-1 in dermal fibroblasts induces collagen fragmentation and functional alterations that resemble aged human skin.
    Aging cell, 2013, Volume: 12, Issue:4

    Topics: Actins; Adenoviridae; Adult; Aged, 80 and over; Cell Shape; Cells, Cultured; Collagen Type I; Dermis; Enzyme Activation; Fibroblasts; Gene Expression Regulation, Enzymologic; HEK293 Cells; Humans; Hydroxamic Acids; Matrix Metalloproteinase 1; Models, Biological; Pyrazines; RNA, Small Interfering; Skin Aging; Sulfonamides; Temperature; Time Factors; Transfection; Young Adult

2013
New matrix metalloproteinase inhibitors based on γ-fluorinated α-aminocarboxylic and α-aminohydroxamic acids.
    Bioorganic & medicinal chemistry, 2015, Jul-01, Volume: 23, Issue:13

    Topics: Binding Sites; Carboxylic Acids; Halogenation; Humans; Hydrogen Bonding; Hydroxamic Acids; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Models, Molecular; Molecular Structure; Protein Binding; Protein Conformation; Pyrazines; Sulfonamides

2015
Developing an Antibody-Drug Conjugate Approach to Selective Inhibition of an Extracellular Protein.
    Chembiochem : a European journal of chemical biology, 2019, 03-15, Volume: 20, Issue:6

    Topics: Animals; Antibodies, Monoclonal, Murine-Derived; Cell Line; Enzyme Assays; Fluorometry; Humans; Hydroxamic Acids; Immunoconjugates; Matrix Metalloproteinase 9; Mice; Protease Inhibitors; Protein Binding; Pyrazines; Sulfonamides

2019