Angewandte Chemie International Edition, ISSN 1433-7851, 09/2016, Volume 55, Issue 39, pp. 11791 - 11796
We report on the design of a polymeric prodrug of the anticancer agent paclitaxel (PTX) by a grafting‐from‐drug approach. A chain transfer agent for reversible...
nanotechnology | paclitaxel | cancer | RAFT polymerization | prodrugs | CREMOPHOR-FREE | PROTEIN | MICELLES | ANTITUMOR-ACTIVITY | CHEMISTRY, MULTIDISCIPLINARY | DELIVERY | NANOPARTICLES | TAXOL | RAFT | Cell Survival - drug effects | Paclitaxel - pharmacology | Paclitaxel - chemical synthesis | Polymers - chemical synthesis | Humans | Paclitaxel - analogs & derivatives | Solubility | Polymerization | Prodrugs - chemistry | Neoplasms - drug therapy | Polymers - pharmacology | Cell Line, Tumor | Hydrophobic and Hydrophilic Interactions | Prodrugs - chemical synthesis | Polymers - chemistry | Prodrugs - pharmacology | Polymer industry | Polymers | Nanotechnology | Paclitaxel
nanotechnology | paclitaxel | cancer | RAFT polymerization | prodrugs | CREMOPHOR-FREE | PROTEIN | MICELLES | ANTITUMOR-ACTIVITY | CHEMISTRY, MULTIDISCIPLINARY | DELIVERY | NANOPARTICLES | TAXOL | RAFT | Cell Survival - drug effects | Paclitaxel - pharmacology | Paclitaxel - chemical synthesis | Polymers - chemical synthesis | Humans | Paclitaxel - analogs & derivatives | Solubility | Polymerization | Prodrugs - chemistry | Neoplasms - drug therapy | Polymers - pharmacology | Cell Line, Tumor | Hydrophobic and Hydrophilic Interactions | Prodrugs - chemical synthesis | Polymers - chemistry | Prodrugs - pharmacology | Polymer industry | Polymers | Nanotechnology | Paclitaxel
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 02/2017, Volume 127, pp. 757 - 770
Antimicrobial research is increasingly being focused on the problem of resistance and biofilm formation. Hamamelitannin (HAM) was recently identified as an...
Scaffold hopping | Antibiotic potentiators | Quorum sensing | Hamamelitannin analogues | MRSA | STAPHYLOCOCCUS-AUREUS PATHOGENESIS | TARGET | ANTIBIOTICS | CHEMISTRY, MEDICINAL | PROTEIN | SUSCEPTIBILITY | QUORUM-SENSING INHIBITOR | DISCOVERY | RIP | POTENTIATORS | Biofilms - drug effects | Methicillin-Resistant Staphylococcus aureus - physiology | User-Computer Interface | Gallic Acid - pharmacology | Methicillin-Resistant Staphylococcus aureus - drug effects | Hexoses - chemical synthesis | Anti-Bacterial Agents - chemical synthesis | Microbial Sensitivity Tests | Anti-Bacterial Agents - chemistry | Drug Design | Gallic Acid - chemical synthesis | Ligands | Anti-Bacterial Agents - pharmacology | Gallic Acid - analogs & derivatives | Drug Evaluation, Preclinical | Gallic Acid - chemistry | Hexoses - chemistry | Hexoses - pharmacology | Care and treatment | Health aspects | Staphylococcus aureus | Staphylococcus aureus infections | Antibacterial agents
Scaffold hopping | Antibiotic potentiators | Quorum sensing | Hamamelitannin analogues | MRSA | STAPHYLOCOCCUS-AUREUS PATHOGENESIS | TARGET | ANTIBIOTICS | CHEMISTRY, MEDICINAL | PROTEIN | SUSCEPTIBILITY | QUORUM-SENSING INHIBITOR | DISCOVERY | RIP | POTENTIATORS | Biofilms - drug effects | Methicillin-Resistant Staphylococcus aureus - physiology | User-Computer Interface | Gallic Acid - pharmacology | Methicillin-Resistant Staphylococcus aureus - drug effects | Hexoses - chemical synthesis | Anti-Bacterial Agents - chemical synthesis | Microbial Sensitivity Tests | Anti-Bacterial Agents - chemistry | Drug Design | Gallic Acid - chemical synthesis | Ligands | Anti-Bacterial Agents - pharmacology | Gallic Acid - analogs & derivatives | Drug Evaluation, Preclinical | Gallic Acid - chemistry | Hexoses - chemistry | Hexoses - pharmacology | Care and treatment | Health aspects | Staphylococcus aureus | Staphylococcus aureus infections | Antibacterial agents
Journal Article
Angewandte Chemie International Edition, ISSN 1433-7851, 05/2016, Volume 55, Issue 22, pp. 6551 - 6555
The modulation of bacterial communication to potentiate the effect of existing antimicrobial drugs is a promising alternative to the development of novel...
quorum sensing | antibiotics | biofilms | potentiators | MRSA | INFECTIONS | SUSCEPTIBILITY | RESISTANCE | INHIBITOR | CHEMISTRY, MULTIDISCIPLINARY | DISCOVERY | Antibiotics | Analysis | Staphylococcus aureus | Genes | Drugs | Chemical communication | Toxicity | Analogue | Cytotoxicity | Infections | Drug development | Antiinfectives and antibacterials | Inhibitors | Modulation | Bacteria | Mammary gland | Detection
quorum sensing | antibiotics | biofilms | potentiators | MRSA | INFECTIONS | SUSCEPTIBILITY | RESISTANCE | INHIBITOR | CHEMISTRY, MULTIDISCIPLINARY | DISCOVERY | Antibiotics | Analysis | Staphylococcus aureus | Genes | Drugs | Chemical communication | Toxicity | Analogue | Cytotoxicity | Infections | Drug development | Antiinfectives and antibacterials | Inhibitors | Modulation | Bacteria | Mammary gland | Detection
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2018, Volume 61, Issue 7, pp. 2753 - 2775
In recent years, thymidylate kinase (TMPK), an enzyme indispensable for bacterial DNA biosynthesis, has been pursued for the development of new antibacterial...
Medicinal Chemistry | Life Sciences | Microbiology and Parasitology | Biomolecules | Biochemistry, Molecular Biology | Chemical Sciences
Medicinal Chemistry | Life Sciences | Microbiology and Parasitology | Biomolecules | Biochemistry, Molecular Biology | Chemical Sciences
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 10/2016, Volume 24, Issue 19, pp. 4563 - 4575
is a frequent cause of biofilm-related infections. Bacterial cells within a biofilm are protected from attack by the immune system and conventional antibiotics...
Antibiotic potentiators | Quorum sensing | Biofilms | Hamamelitannin analogues | Staphylococcus aureus | ANTIBIOTICS | CHEMISTRY, MEDICINAL | BIOCHEMISTRY & MOLECULAR BIOLOGY | SUSCEPTIBILITY | CHEMISTRY, ORGANIC | DISCOVERY | RESISTANCE | AGENTS | Biofilms - drug effects | Staphylococcal Infections - drug therapy | Gallic Acid - pharmacology | Quorum Sensing - drug effects | Staphylococcus aureus - physiology | Humans | Structure-Activity Relationship | Microbial Sensitivity Tests | Anti-Bacterial Agents - chemistry | Vancomycin - pharmacology | Drug Design | Anti-Bacterial Agents - pharmacology | Gallic Acid - analogs & derivatives | Staphylococcus aureus - drug effects | Gallic Acid - chemistry | Hexoses - chemistry | Hexoses - pharmacology | Care and treatment | Health aspects | Antibacterial agents | Analysis | Staphylococcus aureus infections
Antibiotic potentiators | Quorum sensing | Biofilms | Hamamelitannin analogues | Staphylococcus aureus | ANTIBIOTICS | CHEMISTRY, MEDICINAL | BIOCHEMISTRY & MOLECULAR BIOLOGY | SUSCEPTIBILITY | CHEMISTRY, ORGANIC | DISCOVERY | RESISTANCE | AGENTS | Biofilms - drug effects | Staphylococcal Infections - drug therapy | Gallic Acid - pharmacology | Quorum Sensing - drug effects | Staphylococcus aureus - physiology | Humans | Structure-Activity Relationship | Microbial Sensitivity Tests | Anti-Bacterial Agents - chemistry | Vancomycin - pharmacology | Drug Design | Anti-Bacterial Agents - pharmacology | Gallic Acid - analogs & derivatives | Staphylococcus aureus - drug effects | Gallic Acid - chemistry | Hexoses - chemistry | Hexoses - pharmacology | Care and treatment | Health aspects | Antibacterial agents | Analysis | Staphylococcus aureus infections
Journal Article
Forensic Science International, ISSN 0379-0738, 07/2018, Volume 288, pp. 173 - 180
This paper reports the structure elucidation and full characterization of 4-chloromethamphetamine (4-CMA), a compound which was never reported previously...
NPS | Ecstasy | Identification | 4-Chloromethamphetamine (4-CMA) | (Neuro)toxic | Elucidation | BRAIN-SEROTONIN | METABOLISM | RAT | MEDICINE, LEGAL | PARA-CHLOROAMPHETAMINE | Forensic toxicology | Methamphetamine | Ecstasy (Drug) | Research | Identification and classification | Chloromethane | Methods | Neurotoxic agents | Nuclear magnetic resonance--NMR | Tablets | Laboratories | Quantitation | Trifluoroacetyl | Magnetic resonance spectroscopy | Literature reviews | Hydrochloric acid | Neurotoxicity | Drug dosages | Pattern analysis | Public health | Seizing | Serotonin | Health risks | Mass spectroscopy | Liquid chromatography | High-performance liquid chromatography | Gas chromatography | Amphetamines | Dance | Mass spectrometry | High performance liquid chromatography | Structural analysis | Index Medicus
NPS | Ecstasy | Identification | 4-Chloromethamphetamine (4-CMA) | (Neuro)toxic | Elucidation | BRAIN-SEROTONIN | METABOLISM | RAT | MEDICINE, LEGAL | PARA-CHLOROAMPHETAMINE | Forensic toxicology | Methamphetamine | Ecstasy (Drug) | Research | Identification and classification | Chloromethane | Methods | Neurotoxic agents | Nuclear magnetic resonance--NMR | Tablets | Laboratories | Quantitation | Trifluoroacetyl | Magnetic resonance spectroscopy | Literature reviews | Hydrochloric acid | Neurotoxicity | Drug dosages | Pattern analysis | Public health | Seizing | Serotonin | Health risks | Mass spectroscopy | Liquid chromatography | High-performance liquid chromatography | Gas chromatography | Amphetamines | Dance | Mass spectrometry | High performance liquid chromatography | Structural analysis | Index Medicus
Journal Article
Molecular and Cellular Proteomics, ISSN 1535-9476, 12/2014, Volume 13, Issue 12, pp. 3332 - 3342
Probably every cellular process is governed by protein-protein interaction (PPIs), which are often highly dynamic in nature being modulated by in-or external...
YEAST 2-HYBRID SYSTEM | HUMAN-CELLS | DRUG DISCOVERY | REVERSE-TRANSCRIPTASE | BIOCHEMICAL RESEARCH METHODS | DYNAMICS | RECEPTOR | BINDING | INTERACTION TRAP | STRATEGIES | REVEALS | Endoribonucleases - genetics | Phosphorylation | Humans | TYK2 Kinase - metabolism | Arrestins - genetics | Endoplasmic Reticulum Stress - genetics | Arrestins - metabolism | Receptors, Somatostatin - genetics | Receptor, Angiotensin, Type 1 - genetics | Sensitivity and Specificity | HEK293 Cells | Receptors, Somatostatin - metabolism | Protein-Serine-Threonine Kinases - metabolism | STAT3 Transcription Factor - genetics | STAT3 Transcription Factor - metabolism | Endoribonucleases - metabolism | Signal Transduction | Gene Expression Regulation | Protein-Serine-Threonine Kinases - genetics | Benchmarking | Protein Interaction Mapping - methods | Two-Hybrid System Techniques | beta-Arrestins | Receptor, Angiotensin, Type 1 - metabolism | Biosensing Techniques - methods | TYK2 Kinase - genetics | Research
YEAST 2-HYBRID SYSTEM | HUMAN-CELLS | DRUG DISCOVERY | REVERSE-TRANSCRIPTASE | BIOCHEMICAL RESEARCH METHODS | DYNAMICS | RECEPTOR | BINDING | INTERACTION TRAP | STRATEGIES | REVEALS | Endoribonucleases - genetics | Phosphorylation | Humans | TYK2 Kinase - metabolism | Arrestins - genetics | Endoplasmic Reticulum Stress - genetics | Arrestins - metabolism | Receptors, Somatostatin - genetics | Receptor, Angiotensin, Type 1 - genetics | Sensitivity and Specificity | HEK293 Cells | Receptors, Somatostatin - metabolism | Protein-Serine-Threonine Kinases - metabolism | STAT3 Transcription Factor - genetics | STAT3 Transcription Factor - metabolism | Endoribonucleases - metabolism | Signal Transduction | Gene Expression Regulation | Protein-Serine-Threonine Kinases - genetics | Benchmarking | Protein Interaction Mapping - methods | Two-Hybrid System Techniques | beta-Arrestins | Receptor, Angiotensin, Type 1 - metabolism | Biosensing Techniques - methods | TYK2 Kinase - genetics | Research
Journal Article
Bioorganic and Medicinal Chemistry, ISSN 0968-0896, 10/2017, Volume 25, Issue 20, p. 5889
An error is present on page 5175 of the above mentioned published paper. Since we were unable to reproduce the in vitro activity of compound 5 against M....
Journal Article
Forensic Science International, ISSN 0379-0738, 2017, Volume 273, pp. 45 - 52
Highlights • characterization of a new tert -leucinate class synthetic cannabinoid. • GC-EI-MS, HPLC-PDA, LCMS, ESI-HRMS and NMR data for 5F-MDMB-PICA. • First...
Pathology | 5F-MDMB-PICA | Synthetic cannabinoid | GC–MS | NMR | HPLC–PDA | ESI-HRMS | LC–MS
Pathology | 5F-MDMB-PICA | Synthetic cannabinoid | GC–MS | NMR | HPLC–PDA | ESI-HRMS | LC–MS
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 10/2017, Volume 25, Issue 20, pp. 5889 - 5889
Journal Article
Molecules, ISSN 1420-3049, 02/2014, Volume 19, Issue 2, pp. 2571 - 2587
Fourteen new fosmidomycin analogues with altered metal chelating groups were prepared and evaluated for inhibition of E. coli Dxr, M. tuberculosis Dxr and the...
Fosmidomycin | Non-mevalonate pathway | Isoprenoid biosynthesis | Coordination chemistry | DOXP reductoisomerase | Fosfomycin - chemical synthesis | Humans | Plasmodium falciparum - drug effects | Erythrocytes - drug effects | Enzyme Inhibitors - administration & dosage | Antimalarials - administration & dosage | Fosfomycin - administration & dosage | Enzyme Inhibitors - chemistry | Antimalarials - chemistry | Drug Design | Plasmodium falciparum - growth & development | Aldose-Ketose Isomerases - antagonists & inhibitors | Antimalarials - chemical synthesis | Fosfomycin - analogs & derivatives | isoprenoid biosynthesis | non-mevalonate pathway | fosmidomycin | coordination chemistry
Fosmidomycin | Non-mevalonate pathway | Isoprenoid biosynthesis | Coordination chemistry | DOXP reductoisomerase | Fosfomycin - chemical synthesis | Humans | Plasmodium falciparum - drug effects | Erythrocytes - drug effects | Enzyme Inhibitors - administration & dosage | Antimalarials - administration & dosage | Fosfomycin - administration & dosage | Enzyme Inhibitors - chemistry | Antimalarials - chemistry | Drug Design | Plasmodium falciparum - growth & development | Aldose-Ketose Isomerases - antagonists & inhibitors | Antimalarials - chemical synthesis | Fosfomycin - analogs & derivatives | isoprenoid biosynthesis | non-mevalonate pathway | fosmidomycin | coordination chemistry
Journal Article
FORENSIC SCIENCE INTERNATIONAL, ISSN 0379-0738, 04/2017, Volume 273, pp. 45 - 52
A brown powder and different product packages of "spice-like" herbal incenses were analyzed using a systematic identification approach based on liquid...
GC-MS | 5F-MDMB-PICA | Synthetic cannabinoid | HPLC-PDA | LC-MS | NMR | MEDICINE, LEGAL | ESI-HRMS | MDMB-CHMICA | Cannabinoids | Identification | Research | Identification and classification | Designer drugs | Methods | Drugs | Laboratories | Fatalities | Marijuana | Scientific imaging | Mass spectrometry | Emergency communications systems
GC-MS | 5F-MDMB-PICA | Synthetic cannabinoid | HPLC-PDA | LC-MS | NMR | MEDICINE, LEGAL | ESI-HRMS | MDMB-CHMICA | Cannabinoids | Identification | Research | Identification and classification | Designer drugs | Methods | Drugs | Laboratories | Fatalities | Marijuana | Scientific imaging | Mass spectrometry | Emergency communications systems
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2015, Volume 58, Issue 7, pp. 2988 - 3001
Blocking the 2-C-methyl-d-erythrithol-4-phosphate (MEP) pathway for isoprenoid biosynthesis offers interesting prospects for inhibiting Plasmodium or...
MYCOBACTERIUM-TUBERCULOSIS | ANTIMALARIAL-DRUG | DXR INHIBITION | CLINDAMYCIN | CHEMISTRY, MEDICINAL | METHYLERYTHRITOL PHOSPHATE-PATHWAY | ISOPRENOID BIOSYNTHESIS | RESISTANCE | OXA ISOSTERES | 5-PHOSPHATE REDUCTOISOMERASE | NONMEVALONATE PATHWAY | Aldose-Ketose Isomerases - chemistry | Chemistry Techniques, Synthetic | Fosfomycin - chemistry | Escherichia coli - drug effects | Enzyme Inhibitors - pharmacology | Models, Molecular | Crystallography, X-Ray | Structure-Activity Relationship | Plasmodium falciparum - drug effects | Enzyme Inhibitors - chemical synthesis | Molecular Targeted Therapy | Mycobacterium tuberculosis - drug effects | Antimalarials - pharmacology | Microbial Sensitivity Tests | Enzyme Inhibitors - chemistry | Mycobacterium tuberculosis - enzymology | Antimalarials - chemistry | Inhibitory Concentration 50 | Protein Conformation | Aldose-Ketose Isomerases - genetics | Aldose-Ketose Isomerases - antagonists & inhibitors | Aldose-Ketose Isomerases - metabolism | Fosfomycin - analogs & derivatives | Medicinal Chemistry | Basic Medicine | Medical and Health Sciences | Medicin och hälsovetenskap | Läkemedelskemi | Medicinska och farmaceutiska grundvetenskaper
MYCOBACTERIUM-TUBERCULOSIS | ANTIMALARIAL-DRUG | DXR INHIBITION | CLINDAMYCIN | CHEMISTRY, MEDICINAL | METHYLERYTHRITOL PHOSPHATE-PATHWAY | ISOPRENOID BIOSYNTHESIS | RESISTANCE | OXA ISOSTERES | 5-PHOSPHATE REDUCTOISOMERASE | NONMEVALONATE PATHWAY | Aldose-Ketose Isomerases - chemistry | Chemistry Techniques, Synthetic | Fosfomycin - chemistry | Escherichia coli - drug effects | Enzyme Inhibitors - pharmacology | Models, Molecular | Crystallography, X-Ray | Structure-Activity Relationship | Plasmodium falciparum - drug effects | Enzyme Inhibitors - chemical synthesis | Molecular Targeted Therapy | Mycobacterium tuberculosis - drug effects | Antimalarials - pharmacology | Microbial Sensitivity Tests | Enzyme Inhibitors - chemistry | Mycobacterium tuberculosis - enzymology | Antimalarials - chemistry | Inhibitory Concentration 50 | Protein Conformation | Aldose-Ketose Isomerases - genetics | Aldose-Ketose Isomerases - antagonists & inhibitors | Aldose-Ketose Isomerases - metabolism | Fosfomycin - analogs & derivatives | Medicinal Chemistry | Basic Medicine | Medical and Health Sciences | Medicin och hälsovetenskap | Läkemedelskemi | Medicinska och farmaceutiska grundvetenskaper
Journal Article
Scientific Reports, ISSN 2045-2322, 12/2017, Volume 7, Issue 1, pp. 4276 - 18
Invariant Natural Killer T-cells (iNKT-cells) are an attractive target for immune response modulation, as upon CD1d-mediated stimulation with KRN7000, a...
NKT CELLS | RECOGNITION | INKT CELLS | KRN7000 | MULTIDISCIPLINARY SCIENCES | KILLER T-CELLS | BIOLOGICAL EVALUATION | SPHINGOSINE BACKBONE | C-GALACTOSYLCERAMIDE | RECEPTOR | GLYCOLIPIDS | T-cell receptor | CD1d antigen | Immune response | Cytokines | Immunomodulation | Lymphocytes T | Natural killer cells | Galactosylceramide
NKT CELLS | RECOGNITION | INKT CELLS | KRN7000 | MULTIDISCIPLINARY SCIENCES | KILLER T-CELLS | BIOLOGICAL EVALUATION | SPHINGOSINE BACKBONE | C-GALACTOSYLCERAMIDE | RECEPTOR | GLYCOLIPIDS | T-cell receptor | CD1d antigen | Immune response | Cytokines | Immunomodulation | Lymphocytes T | Natural killer cells | Galactosylceramide
Journal Article
Tetrahedron: Asymmetry, ISSN 0957-4166, 2007, Volume 18, Issue 17, pp. 2001 - 2010
Sugar amino acids (SAAs) are carbohydrate derivatives bearing both amino and carboxylic acid functionalities. SAAs are very versatile conformationally biased...
N-LINKED GLYCOPEPTIDES | DIPEPTIDE ISOSTERES | VASOACTIVE-INTESTINAL-PEPTIDE | L-RHAMNOSE | SOLID-PHASE SYNTHESIS | ADENOSINE A RECEPTOR | BUILDING-BLOCKS | CHEMISTRY, PHYSICAL | EFFICIENT S(N)2 REACTIONS | CONFORMATIONAL-ANALYSIS | RECEPTOR-BINDING INHIBITOR
N-LINKED GLYCOPEPTIDES | DIPEPTIDE ISOSTERES | VASOACTIVE-INTESTINAL-PEPTIDE | L-RHAMNOSE | SOLID-PHASE SYNTHESIS | ADENOSINE A RECEPTOR | BUILDING-BLOCKS | CHEMISTRY, PHYSICAL | EFFICIENT S(N)2 REACTIONS | CONFORMATIONAL-ANALYSIS | RECEPTOR-BINDING INHIBITOR
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 12/2010, Volume 285, Issue 51, pp. 40125 - 40134
Proteasomes degrade most proteins in mammalian cells and are established targets of anti-cancer drugs. The majority of proteasome inhibitors are composed of...
20S PROTEASOME | YEAST | CELLS | SELECTIVE INHIBITOR | PROTEIN | MECHANISM | SUBSTRATE | BIOCHEMISTRY & MOLECULAR BIOLOGY | BORTEZOMIB | PEPTIDE | Rabbits | Catalytic Domain | Oligopeptides | Humans | Protease Inhibitors - chemistry | Proteasome Endopeptidase Complex - chemistry | Antineoplastic Agents - chemistry | Sulfones - pharmacology | Protease Inhibitors - pharmacology | Animals | Cytotoxins - pharmacology | Sulfones - chemistry | Cytotoxins - chemistry | HEK293 Cells | Antineoplastic Agents - pharmacology | HeLa Cells | Proteasome Endopeptidase Complex - metabolism | Proteasome Inhibitors | Index Medicus | Ubiquitin | Cysteine Protease | Protease Inhibitor | Protein Degradation | Protein Synthesis and Degradation | Proteasome
20S PROTEASOME | YEAST | CELLS | SELECTIVE INHIBITOR | PROTEIN | MECHANISM | SUBSTRATE | BIOCHEMISTRY & MOLECULAR BIOLOGY | BORTEZOMIB | PEPTIDE | Rabbits | Catalytic Domain | Oligopeptides | Humans | Protease Inhibitors - chemistry | Proteasome Endopeptidase Complex - chemistry | Antineoplastic Agents - chemistry | Sulfones - pharmacology | Protease Inhibitors - pharmacology | Animals | Cytotoxins - pharmacology | Sulfones - chemistry | Cytotoxins - chemistry | HEK293 Cells | Antineoplastic Agents - pharmacology | HeLa Cells | Proteasome Endopeptidase Complex - metabolism | Proteasome Inhibitors | Index Medicus | Ubiquitin | Cysteine Protease | Protease Inhibitor | Protein Degradation | Protein Synthesis and Degradation | Proteasome
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 11/2016, Volume 24, Issue 21, pp. 5172 - 5182
We report the design and synthesis of a series of non-nucleoside TMPK inhibitors ( – ) based on the gram-positive bacterial TMPK inhibitor hit compound . A...
Inhibitors | XDR-TB | Thymine derivatives | Mycobacterium tuberculosis | extensively drug-resistant tuberculosis | Thymidine monophosphate kinase | MYCOBACTERIUM-TUBERCULOSIS | SYSTEM | DESIGN | CHEMISTRY, MEDICINAL | NUCLEOSIDE ANALOGS | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | CHIMERA | POTENT INHIBITORS | DISCOVERY | TMK | ANTIBACTERIAL INHIBITORS | Antitubercular Agents - chemical synthesis | Protein Kinase Inhibitors - chemical synthesis | Piperidines - chemistry | Antitubercular Agents - chemistry | Humans | Nucleoside-Phosphate Kinase - antagonists & inhibitors | Antitubercular Agents - pharmacology | Models, Molecular | Structure-Activity Relationship | Piperidines - chemical synthesis | Mycobacterium tuberculosis - drug effects | Dose-Response Relationship, Drug | Microbial Sensitivity Tests | Protein Kinase Inhibitors - chemistry | Piperidines - pharmacology | Mycobacterium tuberculosis - enzymology | Molecular Structure | Protein Kinase Inhibitors - pharmacology | Nucleoside-Phosphate Kinase - metabolism | Tuberculosis | Nucleosides | Drug resistance in microorganisms | Health aspects | Immunodeficiency | Nucleoside-Phosphate Kinase | Chemical Sciences | Life Sciences | Protein Kinase Inhibitors | Antitubercular Agents | Piperidines
Inhibitors | XDR-TB | Thymine derivatives | Mycobacterium tuberculosis | extensively drug-resistant tuberculosis | Thymidine monophosphate kinase | MYCOBACTERIUM-TUBERCULOSIS | SYSTEM | DESIGN | CHEMISTRY, MEDICINAL | NUCLEOSIDE ANALOGS | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | CHIMERA | POTENT INHIBITORS | DISCOVERY | TMK | ANTIBACTERIAL INHIBITORS | Antitubercular Agents - chemical synthesis | Protein Kinase Inhibitors - chemical synthesis | Piperidines - chemistry | Antitubercular Agents - chemistry | Humans | Nucleoside-Phosphate Kinase - antagonists & inhibitors | Antitubercular Agents - pharmacology | Models, Molecular | Structure-Activity Relationship | Piperidines - chemical synthesis | Mycobacterium tuberculosis - drug effects | Dose-Response Relationship, Drug | Microbial Sensitivity Tests | Protein Kinase Inhibitors - chemistry | Piperidines - pharmacology | Mycobacterium tuberculosis - enzymology | Molecular Structure | Protein Kinase Inhibitors - pharmacology | Nucleoside-Phosphate Kinase - metabolism | Tuberculosis | Nucleosides | Drug resistance in microorganisms | Health aspects | Immunodeficiency | Nucleoside-Phosphate Kinase | Chemical Sciences | Life Sciences | Protein Kinase Inhibitors | Antitubercular Agents | Piperidines
Journal Article
ACS Macro Letters, ISSN 2161-1653, 03/2017, Volume 6, Issue 3, pp. 272 - 276
Acid-sensitive paclitaxel (PTX)–polymer conjugates were designed by applying a grafting-from-drug RAFT approach. PTX was linked through either a cyclic or a...
ACTIVATION | POLYMER SCIENCE | VEHICLES | EFFICACY | DRUG-DELIVERY | PRODRUGS | CREMOPHOR-EL | ACETALS | FORMULATION
ACTIVATION | POLYMER SCIENCE | VEHICLES | EFFICACY | DRUG-DELIVERY | PRODRUGS | CREMOPHOR-EL | ACETALS | FORMULATION
Journal Article
19.
Full Text
Synthesis of extended uridine phosphonates derived from an allosteric p2y2 receptor ligand
Molecules, ISSN 1420-3049, 2014, Volume 19, Issue 4, pp. 4313 - 4325
In this study we report the synthesis of C5/C6-fused uridine phosphonates that are structurally related to earlier reported allosteric P2Y2 receptor ligands. A...
Extended uridine | Nucleoside phosphonates | Astrocytes - cytology | Astrocytes - drug effects | Purinergic P2Y Receptor Agonists - chemical synthesis | Allosteric Regulation | Humans | Uridine - analogs & derivatives | Uridine - pharmacology | Purinergic P2Y Receptor Agonists - pharmacology | Organophosphonates - chemical synthesis | Organophosphonates - pharmacology | Cell Line, Tumor | Receptors, Purinergic P2Y2 - metabolism | Ligands | Quinazolines - chemistry | Uridine - chemical synthesis | Astrocytes - metabolism | nucleoside phosphonates | extended uridine | P2Y2 receptor
Extended uridine | Nucleoside phosphonates | Astrocytes - cytology | Astrocytes - drug effects | Purinergic P2Y Receptor Agonists - chemical synthesis | Allosteric Regulation | Humans | Uridine - analogs & derivatives | Uridine - pharmacology | Purinergic P2Y Receptor Agonists - pharmacology | Organophosphonates - chemical synthesis | Organophosphonates - pharmacology | Cell Line, Tumor | Receptors, Purinergic P2Y2 - metabolism | Ligands | Quinazolines - chemistry | Uridine - chemical synthesis | Astrocytes - metabolism | nucleoside phosphonates | extended uridine | P2Y2 receptor
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 01/2017, Volume 8, Issue 1, pp. 38 - 42
A library of 52 hamamelitannin analogues was synthesized and investigated for its ability to potentiate the effect of vancomycin toward Staphylococcus aureus...
Antibiotic potentiators | Quorum sensing | Biofilms | Hamamelitannin analogues | Staphylococcus aureus | ANTIBIOTICS | CHEMISTRY, MEDICINAL | quorum sensing | SUSCEPTIBILITY | QUORUM-SENSING INHIBITOR | HAMAMELITANNIN ANALOGS | BACTERIAL BIOFILMS | hamamelitannin analogues | STAPHYLOCOCCUS-AUREUS INFECTIONS | RESISTANCE | biofilms
Antibiotic potentiators | Quorum sensing | Biofilms | Hamamelitannin analogues | Staphylococcus aureus | ANTIBIOTICS | CHEMISTRY, MEDICINAL | quorum sensing | SUSCEPTIBILITY | QUORUM-SENSING INHIBITOR | HAMAMELITANNIN ANALOGS | BACTERIAL BIOFILMS | hamamelitannin analogues | STAPHYLOCOCCUS-AUREUS INFECTIONS | RESISTANCE | biofilms
Journal Article