Page last updated: 2024-08-21

thiazoles and largazole

thiazoles has been researched along with largazole in 53 studies

Research

Studies (53)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's11 (20.75)29.6817
2010's38 (71.70)24.3611
2020's4 (7.55)2.80

Authors

AuthorsStudies
Luesch, H; Paul, VJ; Taori, K1
Hong, J; Kim, H; Luesch, H; Taori, K; Ying, Y1
Liu, X; Nasveschuk, CG; Phillips, AJ; Ungermannova, D1
Cramer, N; Kamena, F; Seiser, T1
Bowers, A; Bradner, JE; Schreiber, SL; Taunton, J; West, N; Williams, RM1
Ghosh, AK; Kulkarni, S1
Byeon, SR; Hong, J; Kim, H; Liu, Y; Luesch, H; Ying, Y1
Bowers, AA; Bradner, JE; Estiu, G; Greshock, TJ; Schreiber, SL; West, N; Wiest, O; Williams, RM1
Bowers, AA; Bradner, JE; Newkirk, TL; Schreiber, SL; Troutman-Youngman, AE; West, N; Wiest, O; Williams, RM1
Chen, F; Gao, AH; Li, J; Nan, FJ1
Liu, Y; Luesch, H; Paul, VJ; Taori, K1
Hu, Z; Jiang, S; Li, S; Li, Z; Liao, C; Liu, J; Nicklaus, MC; Yin, B; Zeng, X; Zhou, G1
Altucci, L; Alvarez, R; de Lera, AR; Franci, G; Lepore, I; Pöppler, AC; Souto, JA; Vaz, E1
Morris, JC; Phillips, AJ1
Byeon, S; Hong, J; Kwan, JC; Law, BK; Liu, Y; Luesch, H; Salvador, LA; Ying, Y1
Jiao, XZ; Liu, XY; Wang, LP; Wu, Q; Xiao, Q; Xie, P1
Chen, CS; Forsyth, CJ; Huang, PH; Wang, B1
Benelkebir, H; Crabb, SJ; Ganesan, A; Hayden, AL; Loadman, PM; Lyle, J; Marie, S; Packham, G1
Jiang, S; Li, S; Xu, J; Yao, H1
Boone, MA; Christianson, DW; Cole, KE; Dowling, DP; Phillips, AJ1
Bhansali, P; Casero, RA; Hanigan, CL; Tillekeratne, LM1
Cramer, N1
Diness, F; Fairlie, DP; Nielsen, DS1
Kuchta, RD; Liu, X; Nasveschuk, CG; Parker, SJ; Phillips, AJ; Quade, B; Ungermannova, D; Wang, W; Zhang, G1
Hong, J; Luesch, H1
Friedman, SL; Ji, L; Kwong, S; Lam, W; Li, F; Liu, Y; Lui, EL; Ren, Q; Tang, S; Wang, J; Wang, X; Wang, Z; Xu, Z; Ye, T; Zhang, H; Zhou, S1
Chen, T; Deng, C; Li, FR; Qi, H; Wang, Y; Yan, H; Ye, T; Zhou, S1
Ahmed, S; Beamer, M; Bellini, JV; Bhansali, P; Rahman, A; Riegsecker, S; Tillekeratne, LM1
Fang, X; Jiang, S; Li, E; Liu, Z; Ma, Z; Wang, Y; Xu, L; Zhang, J; Zhang, K; Zhao, Y1
Bowers, AA; Bradner, JE; Estiu, G; Guerra-Bubb, JM; Paranal, R; Smith, WB; Wiest, O; Williams, RM1
Breit, B; Jung, M; Ostrovskyi, D; Schmidtkunz, K; Schotes, C; Senger, J1
Chen, QY; Derendorf, H; Hong, J; Liu, Y; Luesch, H; Salvador, LA; Singh, RS; Sy, SK; Tang, Y; Yu, M1
Chen, J; Jiang, S; Jin, J; Ren, X; Su, SB; Zhou, H1
Byeon, S; Chen, QY; Hong, J; Kim, B; Kwan, JC; Liu, Y; Luesch, H; Park, H; Ryu, S; Salvador, LA; Serrano, PE; Zeller, SL1
Bhansali, P; Casero, RA; Hanigan, CL; Perera, L; Tillekeratne, LM1
Bradner, JE; Charles, B; Clausen, DJ; Gustafson, DL; Hansen, RJ; Lunghofer, PJ; Pilon, JL; Rose, BJ; Thamm, DH; Williams, RM1
Engene, N; Luesch, H; Paul, VJ; Salvador-Reyes, LA1
Christianson, DW; Clausen, DJ; Decroos, C; Haines, BE; Wiest, O; Williams, RM1
Bradner, JE; Clausen, DJ; Haines, BE; Smith, WB; Wiest, O; Williams, RM1
Ballante, F; Chuang, T; Marrocco, B; Marshall, GR; Pirolli, A; Reddy, DN1
Al-Hamashi, AA; Almaliti, J; Casero, RA; Hanigan, CL; Negmeldin, AT; Perera, L; Pflum, MK; Tillekeratne, LM1
Hong, J; Kim, B; Lee, H; Li, C; Luesch, H; Ratnayake, R; Shi, G; Zeller, SL1
Albert, BJ; Barnes, AB; Kyei, GB; Marshall, GR; Niu, A; Ramani, R; Ratner, L; Wender, PA; Williams, RM1
Botta, M; Di Fabio, R; Ferrante, L; Poli, G; Summa, V1
Azofeifa, J; Bunker, EN; Dowell, RD; Garnett, AT; Karman, SS; Liu, X; Richmond, PA; Sanchez, GJ; Toomey, CM; Wheeler, GE; Xu, Q; Zhang, Q1
Bernardes, GJL; Jiménez-Osés, G; Oliveira, BL; Sun, S1
Ermert, P; Luther, A; Obrecht, D; Zbinden, P1
Blanco, MJ1
Lei, X; Li, Y; Ruan, ZW; Shan, G; Yu, X; Zhang, B; Zheng, Y1
Huang, YC; Jiang, S; Liu, J; Lu, YZ; Sun, XY; Wang, GZ; Wang, M; Zhang, KJ; Zhou, GB; Zhou, YC1
Al-Awadhi, FH; Chen, QY; Elsadek, LA; Luesch, H; Ratnayake, R; Salvador-Reyes, LA1
Ding, T; Lei, X; Luo, D; Ruan, ZW; Sui, Q; Zhang, B; Zhu, Y1
Chen, QY; Luesch, H; Qiu, B; Tan, A; Tan, YZ; Wang, X1

Reviews

5 review(s) available for thiazoles and largazole

ArticleYear
Marine natural products: synthetic aspects.
    Natural product reports, 2010, Volume: 27, Issue:8

    Topics: Alkaloids; Biological Products; Depsipeptides; Macrolides; Marine Biology; Molecular Structure; Pyrans; Spiro Compounds; Terpenes; Thiazoles

2010
Synthetic routes and biological evaluation of largazole and its analogues as potent histone deacetylase inhibitors.
    Molecules (Basel, Switzerland), 2011, Jun-07, Volume: 16, Issue:6

    Topics: Depsipeptides; Enzyme Activation; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Thiazoles

2011
Largazole: from discovery to broad-spectrum therapy.
    Natural product reports, 2012, Volume: 29, Issue:4

    Topics: Antineoplastic Agents; Biological Products; Cyanobacteria; Depsipeptides; Histone Deacetylase Inhibitors; Humans; Marine Biology; Molecular Structure; Structure-Activity Relationship; Thiazoles

2012
Largazole Analogues as Histone Deacetylase Inhibitors and Anticancer Agents: An Overview of Structure-Activity Relationships.
    ChemMedChem, 2017, 12-07, Volume: 12, Issue:23

    Topics: Animals; Antineoplastic Agents; Depsipeptides; Dose-Response Relationship, Drug; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Molecular Conformation; Structure-Activity Relationship; Thiazoles

2017
Frontier Between Cyclic Peptides and Macrocycles.
    Methods in molecular biology (Clifton, N.J.), 2019, Volume: 2001

    Topics: Biological Products; Cyclization; Depsipeptides; Humans; Lactones; Macrocyclic Compounds; Oxazoles; Peptide Library; Peptides, Cyclic; Permeability; Protein Conformation; Spiro Compounds; Streptogramins; Thiazoles

2019

Other Studies

48 other study(ies) available for thiazoles and largazole

ArticleYear
Structure and activity of largazole, a potent antiproliferative agent from the Floridian marine cyanobacterium Symploca sp.
    Journal of the American Chemical Society, 2008, Feb-13, Volume: 130, Issue:6

    Topics: Animals; Cell Line, Tumor; Cell Proliferation; Chromatography, High Pressure Liquid; Cyanobacteria; Depsipeptides; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Epithelial Cells; Fibroblasts; Humans; Magnetic Resonance Spectroscopy; Mass Spectrometry; Mice; Molecular Conformation; NIH 3T3 Cells; Reference Standards; Thiazoles

2008
Total synthesis and molecular target of largazole, a histone deacetylase inhibitor.
    Journal of the American Chemical Society, 2008, Jul-02, Volume: 130, Issue:26

    Topics: Antineoplastic Agents; Cyclization; Depsipeptides; Enzyme Inhibitors; Histone Deacetylase Inhibitors; Structure-Activity Relationship; Thiazoles

2008
A concise total synthesis of largazole, solution structure, and some preliminary structure activity relationships.
    Organic letters, 2008, Aug-21, Volume: 10, Issue:16

    Topics: Animals; Cell Line, Tumor; Cell Proliferation; Computer Simulation; Depsipeptides; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Magnetic Resonance Spectroscopy; Mice; Models, Molecular; Molecular Structure; Monte Carlo Method; Solutions; Structure-Activity Relationship; Thiazoles

2008
Synthesis and biological activity of largazole and derivatives.
    Angewandte Chemie (International ed. in English), 2008, Volume: 47, Issue:34

    Topics: 3T3-L1 Cells; Animals; Cell Line, Tumor; Cell Proliferation; Depsipeptides; Humans; Mice; Thiazoles

2008
Total synthesis and biological mode of action of largazole: a potent class I histone deacetylase inhibitor.
    Journal of the American Chemical Society, 2008, Aug-20, Volume: 130, Issue:33

    Topics: Cell Line, Tumor; Cell Proliferation; Depsipeptides; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Histone Deacetylase Inhibitors; Humans; Hydroxamic Acids; Molecular Conformation; Stereoisomerism; Structure-Activity Relationship; Sulfhydryl Compounds; Thiazoles; Vorinostat

2008
Enantioselective total synthesis of (+)-largazole, a potent inhibitor of histone deacetylase.
    Organic letters, 2008, Sep-04, Volume: 10, Issue:17

    Topics: Depsipeptides; Enzyme Inhibitors; Histone Deacetylase Inhibitors; Stereoisomerism; Thiazoles

2008
Synthesis and activity of largazole analogues with linker and macrocycle modification.
    Organic letters, 2008, Sep-18, Volume: 10, Issue:18

    Topics: Cell Line, Tumor; Cell Proliferation; Depsipeptides; Enzyme Inhibitors; Histone Deacetylase Inhibitors; Humans; Thiazoles

2008
Synthesis and conformation-activity relationships of the peptide isosteres of FK228 and largazole.
    Journal of the American Chemical Society, 2009, Mar-04, Volume: 131, Issue:8

    Topics: Catalytic Domain; Depsipeptides; Histone Deacetylase 1; Histone Deacetylase Inhibitors; Humans; Isomerism; Lactams, Macrocyclic; Models, Molecular; Structure-Activity Relationship; Thermodynamics; Thiazoles

2009
Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold.
    Organic letters, 2009, Mar-19, Volume: 11, Issue:6

    Topics: Depsipeptides; Histone Deacetylase Inhibitors; Marine Biology; Models, Molecular; Molecular Structure; Structure-Activity Relationship; Thiazoles; Zinc

2009
Synthesis and biological evaluation of c7-demethyl largazole analogues.
    ChemMedChem, 2009, Volume: 4, Issue:8

    Topics: Antineoplastic Agents; Binding Sites; Cell Line, Tumor; Computer Simulation; Depsipeptides; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Recombinant Proteins; Structure-Activity Relationship; Thiazoles

2009
Combinatorial strategies by marine cyanobacteria: symplostatin 4, an antimitotic natural dolastatin 10/15 hybrid that synergizes with the coproduced HDAC inhibitor largazole.
    Chembiochem : a European journal of chemical biology, 2009, Jul-06, Volume: 10, Issue:10

    Topics: Antimicrobial Cationic Peptides; Antimitotic Agents; Antineoplastic Combined Chemotherapy Protocols; Cell Cycle; Cell Line, Tumor; Cyanobacteria; Depsipeptides; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Peptides; Thiazoles

2009
Total synthesis and biological evaluation of largazole and derivatives with promising selectivity for cancers cells.
    Organic letters, 2010, Mar-19, Volume: 12, Issue:6

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Crystallography, X-Ray; Depsipeptides; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Molecular Conformation; Stereoisomerism; Structure-Activity Relationship; Substrate Specificity; Thiazoles

2010
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
    Journal of medicinal chemistry, 2010, Jun-24, Volume: 53, Issue:12

    Topics: Acetylation; Antineoplastic Agents; Apoptosis; CD11c Antigen; Cell Differentiation; Cell Line, Tumor; Cyclin-Dependent Kinase Inhibitor p21; Depsipeptides; Drug Screening Assays, Antitumor; Granulocytes; Histone Deacetylase 1; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Recombinant Proteins; Repressor Proteins; Stereoisomerism; Structure-Activity Relationship; Thiazoles; Tubulin

2010
Anticolon cancer activity of largazole, a marine-derived tunable histone deacetylase inhibitor.
    The Journal of pharmacology and experimental therapeutics, 2010, Volume: 335, Issue:2

    Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Cycle; Cell Line, Tumor; Cell Survival; Chromatography, High Pressure Liquid; Colonic Neoplasms; Depsipeptides; Down-Regulation; Drug Stability; Female; Gene Expression Regulation, Enzymologic; Gene Expression Regulation, Neoplastic; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Immunohistochemistry; Mass Spectrometry; Mice; Mice, Nude; Molecular Structure; Oligonucleotide Array Sequence Analysis; Recombinant Proteins; Reverse Transcriptase Polymerase Chain Reaction; Thiazoles; Xenograft Model Antitumor Assays

2010
Concise total synthesis of largazole.
    Journal of Asian natural products research, 2010, Volume: 12, Issue:11

    Topics: Catalysis; Depsipeptides; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Thiazoles; Thiazolidines

2010
Total syntheses of the histone deacetylase inhibitors largazole and 2-epi-largazole: application of N-heterocyclic carbene mediated acylations in complex molecule synthesis.
    The Journal of organic chemistry, 2011, Feb-18, Volume: 76, Issue:4

    Topics: Acylation; Biological Products; Cell Line, Tumor; Cell Survival; Depsipeptides; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Heterocyclic Compounds; Histone Deacetylase Inhibitors; Humans; Male; Methane; Stereoisomerism; Structure-Activity Relationship; Thiazoles

2011
Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability.
    Bioorganic & medicinal chemistry, 2011, Jun-15, Volume: 19, Issue:12

    Topics: Animals; Antineoplastic Agents; Blotting, Western; Cell Line, Tumor; Cell Proliferation; Depsipeptides; Drug Stability; Enzyme Activation; HeLa Cells; Histone Deacetylase Inhibitors; Humans; Mice; Molecular Structure; Structure-Activity Relationship; Thiazoles

2011
Structural basis of the antiproliferative activity of largazole, a depsipeptide inhibitor of the histone deacetylases.
    Journal of the American Chemical Society, 2011, Aug-17, Volume: 133, Issue:32

    Topics: Crystallography, X-Ray; Cyanobacteria; Depsipeptides; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Models, Molecular; Repressor Proteins; Thiazoles

2011
Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: synthesis and biological evaluation.
    Journal of medicinal chemistry, 2011, Nov-10, Volume: 54, Issue:21

    Topics: Acetylation; Antineoplastic Agents; Binding Sites; Cell Proliferation; Chelating Agents; Depsipeptides; Drug Screening Assays, Antitumor; HCT116 Cells; HeLa Cells; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Isoenzymes; Stereoisomerism; Structure-Activity Relationship; Thiazoles; Zinc

2011
Catalytic asymmetric functionalization of inert bonds and synthesis of bioactive natural products.
    Chimia, 2011, Volume: 65, Issue:9

    Topics: Biological Products; Catalysis; Depsipeptides; Hydrogen Bonding; Molecular Structure; Sesquiterpenes; Stereoisomerism; Thiazoles

2011
Synthesis of the thiazole-thiazoline fragment of largazole analogues.
    The Journal of organic chemistry, 2011, Dec-02, Volume: 76, Issue:23

    Topics: Depsipeptides; Molecular Structure; Stereoisomerism; Thiazoles

2011
Largazole and its derivatives selectively inhibit ubiquitin activating enzyme (e1).
    PloS one, 2012, Volume: 7, Issue:1

    Topics: Adenine; Animals; Cell Line; Cyclin-Dependent Kinase Inhibitor p27; Depsipeptides; Dose-Response Relationship, Drug; Electrophoresis, Polyacrylamide Gel; Enzyme Activation; Green Fluorescent Proteins; HEK293 Cells; Humans; Immunoblotting; Molecular Structure; Telomeric Repeat Binding Protein 1; Thiazoles; Transfection; Ubiquitin; Ubiquitin-Activating Enzymes; Ubiquitination

2012
A histone deacetylase inhibitor, largazole, decreases liver fibrosis and angiogenesis by inhibiting transforming growth factor-β and vascular endothelial growth factor signalling.
    Liver international : official journal of the International Association for the Study of the Liver, 2013, Volume: 33, Issue:4

    Topics: Acetylation; Angiogenesis Inhibitors; Animals; Apoptosis; Carbon Tetrachloride; Cell Line; Depsipeptides; Dose-Response Relationship, Drug; Hepatic Stellate Cells; Histone Deacetylase Inhibitors; Histone Deacetylases; Histones; Humans; Liver; Liver Cirrhosis, Experimental; Male; Mice; Mice, Inbred BALB C; Neovascularization, Physiologic; Rats; RNA Interference; Signal Transduction; Thiazoles; Time Factors; Transfection; Transforming Growth Factor beta; Vascular Endothelial Growth Factor A

2013
Role of histone deacetylase inhibitors in the aging of human umbilical cord mesenchymal stem cells.
    Journal of cellular biochemistry, 2013, Volume: 114, Issue:10

    Topics: Apoptosis; Cell Proliferation; Cells, Cultured; Cellular Senescence; Chromatin Immunoprecipitation; Depsipeptides; Histone Deacetylase Inhibitors; Humans; Hydroxamic Acids; Mesenchymal Stem Cells; Real-Time Polymerase Chain Reaction; Thiazoles; Umbilical Cord

2013
Largazole, a class I histone deacetylase inhibitor, enhances TNF-α-induced ICAM-1 and VCAM-1 expression in rheumatoid arthritis synovial fibroblasts.
    Toxicology and applied pharmacology, 2013, Jul-15, Volume: 270, Issue:2

    Topics: Arthritis, Rheumatoid; Blotting, Western; Depsipeptides; Drug Synergism; Fibroblasts; Histone Deacetylase Inhibitors; Humans; Intercellular Adhesion Molecule-1; Matrix Metalloproteinase 2; Oncogene Protein v-akt; p38 Mitogen-Activated Protein Kinases; Recombinant Proteins; Reverse Transcriptase Polymerase Chain Reaction; RNA; Synovial Membrane; Thiazoles; Tumor Necrosis Factor-alpha; Vascular Cell Adhesion Molecule-1

2013
Comprehensive analysis for histone acetylation of human colon cancer cells treated with a novel HDAC inhibitor.
    Current pharmaceutical design, 2014, Volume: 20, Issue:11

    Topics: Acetylation; Antineoplastic Agents; Colonic Neoplasms; Depsipeptides; Epigenesis, Genetic; HCT116 Cells; Histone Deacetylase Inhibitors; Histone Deacetylases; Histones; Humans; Isotope Labeling; Thiazoles

2014
Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs.
    Bioorganic & medicinal chemistry letters, 2013, Nov-01, Volume: 23, Issue:21

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Survival; Depsipeptides; Histone Deacetylase Inhibitors; Humans; Molecular Docking Simulation; Neoplasms; Oxazoles; Thiazoles

2013
Total synthesis of (18S)- and (18R)-homolargazole by rhodium-catalyzed hydrocarboxylation.
    Chemistry (Weinheim an der Bergstrasse, Germany), 2014, Feb-17, Volume: 20, Issue:8

    Topics: Alkadienes; Catalysis; Depsipeptides; Ligands; Molecular Structure; Rhodium; Stereoisomerism; Thiazoles

2014
Largazole pharmacokinetics in rats by LC-MS/MS.
    Marine drugs, 2014, Mar-20, Volume: 12, Issue:3

    Topics: Animals; Chromatography, High Pressure Liquid; Depsipeptides; Half-Life; Histone Deacetylase Inhibitors; Humans; Indicators and Reagents; Male; Mass Spectrometry; Plasma; Protein Binding; Quality Control; Rats; Rats, Sprague-Dawley; Reproducibility of Results; Thiazoles

2014
Largazole, an inhibitor of class I histone deacetylases, attenuates inflammatory corneal neovascularization.
    European journal of pharmacology, 2014, Oct-05, Volume: 740

    Topics: ADAM Proteins; Animals; Anti-Inflammatory Agents; Cell Line; Cell Movement; Cell Proliferation; Corneal Neovascularization; Depsipeptides; Endothelial Cells; Epidermal Growth Factor; Female; Fibroblast Growth Factors; Histone Deacetylase Inhibitors; Humans; Mice, Inbred BALB C; RNA, Messenger; Thiazoles; Thrombospondin 1; Thrombospondins; Transforming Growth Factor beta1; Vascular Endothelial Growth Factor A

2014
Evaluation of class I HDAC isoform selectivity of largazole analogues.
    Bioorganic & medicinal chemistry letters, 2014, Aug-15, Volume: 24, Issue:16

    Topics: Depsipeptides; Dose-Response Relationship, Drug; Histone Deacetylase 1; Histone Deacetylase Inhibitors; Humans; Isoenzymes; Molecular Structure; Structure-Activity Relationship; Thiazoles

2014
Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups.
    European journal of medicinal chemistry, 2014, Oct-30, Volume: 86

    Topics: Depsipeptides; Dose-Response Relationship, Drug; HCT116 Cells; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Models, Molecular; Molecular Structure; Structure-Activity Relationship; Thiazoles

2014
Comparative pharmacokinetic properties and antitumor activity of the marine HDACi Largazole and Largazole peptide isostere.
    Cancer chemotherapy and pharmacology, 2015, Volume: 75, Issue:4

    Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Cycle Checkpoints; Depsipeptides; Dose-Response Relationship, Drug; Female; Histone Deacetylase Inhibitors; Humans; Kaplan-Meier Estimate; Lung Neoplasms; Mice; Mice, Nude; Models, Biological; Molecular Structure; Pyridines; Structure-Activity Relationship; Thiazoles; Xenograft Model Antitumor Assays

2015
Targeted natural products discovery from marine cyanobacteria using combined phylogenetic and mass spectrometric evaluation.
    Journal of natural products, 2015, Mar-27, Volume: 78, Issue:3

    Topics: Biological Products; Chromatography, High Pressure Liquid; Colonic Neoplasms; Cyanobacteria; Cytotoxins; Depsipeptides; HCT116 Cells; Humans; Marine Biology; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Phylogeny; Thiazoles

2015
Variable active site loop conformations accommodate the binding of macrocyclic largazole analogues to HDAC8.
    Biochemistry, 2015, Mar-31, Volume: 54, Issue:12

    Topics: Catalytic Domain; Crystallography, X-Ray; Depsipeptides; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Models, Molecular; Molecular Dynamics Simulation; Mutagenesis, Site-Directed; Protein Conformation; Recombinant Proteins; Repressor Proteins; Thiazoles

2015
Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole.
    Bioorganic & medicinal chemistry, 2015, Aug-01, Volume: 23, Issue:15

    Topics: Binding Sites; Cell Line, Tumor; Cell Survival; Depsipeptides; Drug Design; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Molecular Docking Simulation; Protein Structure, Tertiary; Pyridines; Structure-Activity Relationship; Thiazoles

2015
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
    Journal of medicinal chemistry, 2016, Feb-25, Volume: 59, Issue:4

    Topics: Depsipeptides; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Molecular Docking Simulation; Protein Isoforms; Structure-Activity Relationship; Thiazoles

2016
Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue.
    Journal of medicinal chemistry, 2016, 12-08, Volume: 59, Issue:23

    Topics: Depsipeptides; Dose-Response Relationship, Drug; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Molecular Dynamics Simulation; Molecular Structure; Structure-Activity Relationship; Thiazoles

2016
Synthesis and biological evaluation of largazole zinc-binding group analogs.
    Bioorganic & medicinal chemistry, 2017, 06-15, Volume: 25, Issue:12

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Survival; Depsipeptides; Histone Deacetylase 1; Histone Deacetylase Inhibitors; Humans; Molecular Docking Simulation; Neoplasms; Structure-Activity Relationship; Thiazoles; Zinc

2017
Combinations of isoform-targeted histone deacetylase inhibitors and bryostatin analogues display remarkable potency to activate latent HIV without global T-cell activation.
    Scientific reports, 2017, 08-07, Volume: 7, Issue:1

    Topics: Bryostatins; CD4-Positive T-Lymphocytes; Cell Line; Depsipeptides; Drug Synergism; Drug Therapy, Combination; HeLa Cells; Histone Deacetylase 1; Histone Deacetylase Inhibitors; HIV-1; Humans; Jurkat Cells; Lymphocyte Activation; Molecular Structure; Thiazoles; Virus Activation; Virus Latency

2017
Genome-wide dose-dependent inhibition of histone deacetylases studies reveal their roles in enhancer remodeling and suppression of oncogenic super-enhancers.
    Nucleic acids research, 2018, 02-28, Volume: 46, Issue:4

    Topics: Acetylation; Cell Line; Cell Line, Transformed; Cytostatic Agents; Depsipeptides; Dose-Response Relationship, Drug; Enhancer Elements, Genetic; Genome; Histone Code; Histone Deacetylase Inhibitors; Histone Deacetylases; Histones; Oncogenes; Promoter Regions, Genetic; RNA Polymerase II; RNA, Messenger; Thiazoles

2018
Radical-Mediated Thiol-Ene Strategy: Photoactivation of Thiol-Containing Drugs in Cancer Cells.
    Angewandte Chemie (International ed. in English), 2018, 11-26, Volume: 57, Issue:48

    Topics: Alkenes; Cell Survival; Depsipeptides; Dose-Response Relationship, Drug; Free Radicals; HCT116 Cells; Histone Deacetylase Inhibitors; Humans; Molecular Structure; Photochemical Processes; Structure-Activity Relationship; Sulfhydryl Compounds; Thiazoles; Ultraviolet Rays

2018
Building upon Nature's Framework: Overview of Key Strategies Toward Increasing Drug-Like Properties of Natural Product Cyclopeptides and Macrocycles.
    Methods in molecular biology (Clifton, N.J.), 2019, Volume: 2001

    Topics: Anthraquinones; Biological Availability; Biological Products; Chemistry, Pharmaceutical; Cyclosporine; Cyclotides; Daptomycin; Depsipeptides; Drug Design; Drug Discovery; Ethers, Cyclic; Gramicidin; Lipopeptides; Macrocyclic Compounds; Macrolides; omega-Conotoxins; Organophosphorus Compounds; Oxazoles; Peptides; Peptides, Cyclic; Thiazoles; Thiazolidines

2019
Synthesis and Preliminary Biological Evaluation of Two Fluoroolefin Analogs of Largazole Inspired by the Structural Similarity of the Side Chain Unit in Psammaplin A.
    Marine drugs, 2019, Jun-03, Volume: 17, Issue:6

    Topics: Alkenes; Aquatic Organisms; Cyanobacteria; Depsipeptides; Disulfides; Enzyme Activation; Histone Deacetylase Inhibitors; Histone Deacetylases; Thiazoles; Tyrosine

2019
Suppression of Musashi‑2 by the small compound largazole exerts inhibitory effects on malignant cells.
    International journal of oncology, 2020, Volume: 56, Issue:5

    Topics: Adult; Aged; Animals; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Proliferation; Cell Survival; Depsipeptides; Female; Gene Expression Regulation, Neoplastic; Humans; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Lung Neoplasms; Male; Mice; Middle Aged; Models, Molecular; Molecular Docking Simulation; Protein Conformation; RNA-Binding Proteins; Thiazoles; Up-Regulation

2020
Largazole is a Brain-Penetrant Class I HDAC Inhibitor with Extended Applicability to Glioblastoma and CNS Diseases.
    ACS chemical neuroscience, 2020, 07-01, Volume: 11, Issue:13

    Topics: Animals; Brain; Cell Line, Tumor; Central Nervous System Diseases; Depsipeptides; Glioblastoma; Histone Deacetylase Inhibitors; Mice; Thiazoles

2020
Unexpected Enhancement of HDACs Inhibition by MeS Substitution at C-2 Position of Fluoro Largazole.
    Marine drugs, 2020, Jun-30, Volume: 18, Issue:7

    Topics: Depsipeptides; Histone Deacetylase Inhibitors; Histone Deacetylases; Molecular Structure; Structure-Activity Relationship; Thiazoles

2020
Largazole Inhibits Ocular Angiogenesis by Modulating the Expression of VEGFR2 and p21.
    Marine drugs, 2021, Aug-22, Volume: 19, Issue:8

    Topics: Angiogenesis Inhibitors; Animals; Aquatic Organisms; Cyanobacteria; Depsipeptides; Disease Models, Animal; Endothelial Cells; Eye; Eye Diseases; Female; Humans; Male; Mice; Mice, Inbred C57BL; Neovascularization, Pathologic; Phytotherapy; Thiazoles; Vascular Endothelial Growth Factor Receptor-2

2021