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Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2018, Volume 61, Issue 8, pp. 3503 - 3515
A series of novel hydrogen peroxide sensitive prodrugs of methotrexate (MTX) and aminopterin (AMT) were synthesized and evaluated for therapeutic efficacy in... 
COLLAGEN-INDUCED ARTHRITIS | CROSS-LINKING AGENTS | THERAPEUTIC SUPPRESSION | OXIDATIVE STRESS | CHEMISTRY, MEDICINAL | FOLIC-ACID ANTAGONISTS | INTRAARTICULAR DELIVERY | DRUG-DELIVERY | IN-VIVO | TISSUE REACTIVITY | ANTICANCER PRODRUGS | Boronic Acids - toxicity | Aminopterin - therapeutic use | Arthritis, Experimental - drug therapy | Humans | Methotrexate - pharmacokinetics | Microsomes, Liver - metabolism | Male | Methotrexate - toxicity | Methotrexate - therapeutic use | Boronic Acids - therapeutic use | Arthritis, Experimental - metabolism | Collagen Type II - metabolism | Hydrogen Peroxide - chemistry | Arthritis, Rheumatoid - metabolism | MCF-7 Cells | Arthritis, Experimental - chemically induced | Arthritis, Rheumatoid - drug therapy | Antirheumatic Agents - chemical synthesis | Mice, Inbred DBA | Boronic Acids - chemical synthesis | Antirheumatic Agents - therapeutic use | Solubility | Aminopterin - pharmacokinetics | Arthritis, Rheumatoid - chemically induced | Hydrogen Peroxide - metabolism | Antirheumatic Agents - toxicity | Animals | Aminopterin - toxicity | Prodrugs - pharmacokinetics | Boronic Acids - pharmacokinetics | Prodrugs - toxicity | Prodrugs - chemical synthesis | Antirheumatic Agents - pharmacokinetics | Prodrugs - therapeutic use | Aminopterin - chemical synthesis | Methotrexate - analogs & derivatives | Index Medicus
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 08/2013, Volume 66, pp. 135 - 145
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 2006, Volume 14, Issue 24, pp. 8608 - 8621
In order to produce potent new leads for anticancer drugs, a new series of quinazoline analogs was designed to resemble methotrexate (MTX, ) structure features... 
Antitumor activity | DHFR inhibitors | 4(3 H)-Quinazolinone | Molecular modeling studies | 4(3H)-Quinazolinone | CHEMISTRY, MEDICINAL | BIOCHEMISTRY & MOLECULAR BIOLOGY | DRUG DISCOVERY | METHOTREXATE | CHEMISTRY, ORGANIC | NATIONAL-CANCER-INSTITUTE | 4(3H)-quinazolinone | TRIMETREXATE | PNEUMOCYSTIS-CARINII | antitumor activity | PHARMACOLOGY | molecular modeling studies | BIOLOGICAL EVALUATION | FORCE-FIELD | PART 2 | CYTOTOXICITY | Methotrexate - pharmacology | Folic Acid Antagonists - chemistry | Lung Neoplasms - drug therapy | Liver - enzymology | Tetrahydrofolate Dehydrogenase - chemistry | Antineoplastic Agents - chemical synthesis | Humans | Lung Neoplasms - pathology | Structure-Activity Relationship | Enzyme Inhibitors - chemical synthesis | Cattle | Enzyme Inhibitors - chemistry | Antineoplastic Agents - pharmacology | Molecular Structure | Folic Acid Antagonists - chemical synthesis | Quinazolinones - pharmacology | Tumor Cells, Cultured - drug effects | Enzyme Inhibitors - pharmacology | Models, Molecular | Antineoplastic Agents - chemistry | Breast Neoplasms - drug therapy | Quinazolinones - chemical synthesis | Animals | Breast Neoplasms - pathology | Cell Proliferation - drug effects | Quinazolinones - chemistry | Folic Acid Antagonists - pharmacology | Models | Dihydrofolate reductase | Analysis | Pharmacy
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 07/2015, Volume 23, Issue 13, pp. 3059 - 3080
Osteoarthritis and rheumatoid arthritis are the two most common types of arthritis. Cartilage breakdown is a key feature of both diseases which contributes to... 
Disease-modifying anti-rheumatic drugs | Cyclooxygenase | Kinase | Natural products | Rheumatoid arthritis | Methotrexate | Osteoarthritis | Non-steroidal anti-inflammatory drugs | Nutraceuticals | COLLAGEN-INDUCED ARTHRITIS | MODIFYING ANTIRHEUMATIC DRUGS | CHEMISTRY, MEDICINAL | ACTIVE RHEUMATOID-ARTHRITIS | BIOCHEMISTRY & MOLECULAR BIOLOGY | METHOTREXATE DERIVATIVES BEARING | CHEMISTRY, ORGANIC | RANDOMIZED CONTROLLED-TRIAL | CONTROLLED CLINICAL-TRIAL | BOSWELLIA-SERRATA EXTRACT | MATRIX METALLOPROTEINASE-13 INHIBITORS | PLACEBO-CONTROLLED TRIAL | NF-KAPPA-B | Glucocorticoids - chemical synthesis | Glucocorticoids - therapeutic use | Analgesics, Opioid - chemical synthesis | Cartilage - pathology | Humans | Drugs, Investigational - therapeutic use | Cartilage - drug effects | Methotrexate - therapeutic use | Osteoarthritis - drug therapy | Joints - physiopathology | Osteoarthritis - physiopathology | Methotrexate - chemical synthesis | Arthritis, Rheumatoid - drug therapy | Antirheumatic Agents - chemical synthesis | Osteoarthritis - pathology | Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis | Arthritis, Rheumatoid - physiopathology | Antirheumatic Agents - therapeutic use | Biological Products - therapeutic use | Drugs, Investigational - chemical synthesis | Pain - prevention & control | Joints - drug effects | Analgesics, Opioid - therapeutic use | Joints - pathology | Cartilage - physiopathology | Pain - pathology | Biological Products - isolation & purification | Arthritis, Rheumatoid - pathology | Biological Products - chemistry | Anti-Inflammatory Agents, Non-Steroidal - therapeutic use | Pain - physiopathology | Antiarthritic agents | Arthritis | Rheumatoid factor | Corticosteroids | Fluocinolone acetonide | Functional foods | Opioids | Development and progression
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 05/2018, Volume 26, Issue 9, pp. 2674 - 2685
Bridge homologation of the previously reported nonclassical two-carbon-bridged antifolate, 2,4-diamino-6-phenethylpyrido[3,2- ]pyrimidine ( ), afforded the... 
DHFR | Molecular docking study | Nonclassical antifolates | Antitumor | ANTIFOLATE RESISTANCE | ANTIPROLIFERATIVE ACTIVITY | CHEMISTRY, MEDICINAL | MECHANISM | REDUCED FOLATE CARRIER | ANALOGS | THYMIDYLATE SYNTHASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | RECEPTOR | CANCER | POTENTIAL ANTICANCER AGENTS | THIOREDOXIN REDUCTASE | Methotrexate - pharmacology | Folic Acid Antagonists - chemistry | Up-Regulation | Tetrahydrofolate Dehydrogenase - chemistry | Apoptosis - drug effects | Pyridines - chemistry | Pyrimidines - chemical synthesis | Antineoplastic Agents - chemical synthesis | Humans | Pyrimidines - chemistry | Drug Design | Antineoplastic Agents - pharmacology | Molecular Structure | Folic Acid Antagonists - chemical synthesis | Recombinant Proteins - metabolism | Catalytic Domain | Pyridines - chemical synthesis | Pyrimidines - pharmacology | Antineoplastic Agents - chemistry | Blotting, Western | Tetrahydrofolate Dehydrogenase - metabolism | Hydrogen Bonding | Cell Line, Tumor | Molecular Docking Simulation | Pyridines - pharmacology | S Phase Cell Cycle Checkpoints - drug effects | Folic Acid Antagonists - pharmacology | Drug Screening Assays, Antitumor | Tetrahydrofolate Dehydrogenase - genetics | Antimitotic agents | Pyrimidines | Dihydrofolate reductase | Antineoplastic agents | Analysis
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 01/2017, Volume 60, Issue 2, pp. 767 - 786
By use of a structure-based computational method for identification of structurally novel Janus kinase (JAK) inhibitors predicted to bind beyond the ATP... 
PLACEBO | CHEMISTRY, MEDICINAL | CHRONIC PLAQUE PSORIASIS | EFFICACY | ACTIVE RHEUMATOID-ARTHRITIS | PHASE-III | METHOTREXATE | OPEN-LABEL | COMBINATION | TOFACITINIB CP-690,550 | DISCOVERY | Phosphorylation | Indazoles - chemical synthesis | Humans | Microsomes, Liver - metabolism | Crystallography, X-Ray | Administration, Cutaneous | Hepatocytes - metabolism | Indazoles - administration & dosage | Lung Diseases - drug therapy | Janus Kinase 3 - antagonists & inhibitors | Heterocyclic Compounds, 2-Ring - toxicity | Drug Design | Anti-Inflammatory Agents - administration & dosage | Binding Sites | Janus Kinase 2 - antagonists & inhibitors | Protein Kinase Inhibitors - chemical synthesis | Anti-Inflammatory Agents - pharmacology | Anti-Inflammatory Agents - toxicity | Heterocyclic Compounds, 2-Ring - administration & dosage | Solubility | Administration, Inhalation | Rats | Skin Diseases - drug therapy | Janus Kinase 1 - antagonists & inhibitors | Heterocyclic Compounds, 2-Ring - pharmacology | Indazoles - pharmacology | Janus Kinases - antagonists & inhibitors | Protein Kinase Inhibitors - administration & dosage | Animals | Indazoles - toxicity | Dogs | Protein Kinase Inhibitors - toxicity | Anti-Inflammatory Agents - chemical synthesis | Mice, Inbred BALB C | Protein Kinase Inhibitors - pharmacology | Heterocyclic Compounds, 2-Ring - chemical synthesis | Index Medicus
Journal Article
Journal Article
Journal Article
Journal Article
Journal of Heterocyclic Chemistry, ISSN 0022-152X, 04/2019, Volume 56, Issue 4, pp. 1352 - 1361
Considering pteridine as a worthy structure for improving probes of magnificent therapeutic potentials, some new pteridine conjugates were synthesized by... 
AZOLE | DESIGN | DNA | BIOLOGICAL-ACTIVITY | METHOTREXATE | CHEMISTRY, ORGANIC | ANTITUMOR-ACTIVITY | FACILE | MICROWAVE-ASSISTED SYNTHESIS | DERIVATIVES | TNBS-INDUCED COLITIS | Pyrimidines | Aromatic amines | Analysis | Formaldehyde
Journal Article
Journal Article