Search Results - "Carme, Masdeu"
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Recent advances of the Povarov reaction in medicinal chemistry
Published in Drug discovery today. Technologies (01-11-2018)“…[Display omitted] The Povarov multicomponent reaction consists on the condensation of an aniline, an aldehyde, and an activated olefin to generate a…”
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Fused 1,5-Naphthyridines: Synthetic Tools and Applications
Published in Molecules (Basel, Switzerland) (31-07-2020)“…Heterocyclic nitrogen compounds, including fused 1,5-naphthyridines, have versatile applications in the fields of synthetic organic chemistry and play an…”
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Synthetic Strategies, Reactivity and Applications of 1,5-Naphthyridines
Published in Molecules (Basel, Switzerland) (16-07-2020)“…This review covers the synthesis and reactivity of 1,5-naphthyridine derivatives published in the last 18 years. These heterocycles present a significant…”
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Gel-Free Tools for Quick and Simple Screening of Anti-Topoisomerase 1 Compounds
Published in Pharmaceuticals (Basel, Switzerland) (27-04-2023)“…With the increasing need for effective compounds against cancer or pathogen-borne diseases, the development of new tools to investigate the enzymatic activity…”
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Highly Enantioselective Conjugate Additions of Aldehydes to Vinyl Sulfones
Published in Chemistry : a European journal (02-02-2009)“…Joined together, organocatalysts aldehydes and sulfones: A diaryl prolinol silyl ether was found to catalyse efficiently and enantioselectively the conjugate…”
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In vitro and in vivo activity of a new small-molecule inhibitor of HDAC6 in mantle cell lymphoma
Published in Haematologica (Roma) (01-11-2018)“…Cancer origin and development is associated not only with genetic alterations, but also with the disturbance of epigenetic profiles.1 In this regard, the…”
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Efficient AntiMycolata Agents by Increasing the Lipophilicity of Known Antibiotics through Multicomponent Reactions
Published in Antibiotics (Basel) (03-01-2023)“…New antibiotic agents were prepared using Povarov and Ugi multicomponent reactions upon the known drugs sulfadoxine and dapsone. The prepared derivatives, with…”
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A patent review of topoisomerase I inhibitors (2016-present)
Published in Expert opinion on therapeutic patents (03-06-2021)“…Topoisomerases are important targets for therapeutic improvement in the treatment of some diseases, including cancer. Inhibitors and poisons of topoisomerase I…”
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The Intramolecular Povarov Tool in the Construction of Fused Nitrogen-Containing Heterocycles
Published in Topics in current chemistry (2016) (01-06-2023)“…Nitrogen heterocycles are part of the structure of natural products and agents with important biological activity, such as antiviral, antibiotic, and antitumor…”
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Formation of γ-Oxoacids and 1 H -Pyrrol-2(5 H )-ones from α,β-Unsaturated Ketones and Ethyl Nitroacetate
Published in Journal of organic chemistry (05-11-2010)Get full text
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Abstract 4725: Efficacy of a new small-molecule inhibitor of histone deacetylase 6 (HDAC6) in preclinical models of B-cell lymphoma and acute myeloid leukemia
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Histone deacetylase 6 (HDAC6) is a protein modifier that is an increasingly attractive pharmacological target. Interestingly, the observation that the HDAC6…”
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Formation of γ-Oxoacids and 1H-Pyrrol-2(5H)-ones from α,β-Unsaturated Ketones and Ethyl Nitroacetate
Published in Journal of organic chemistry (05-11-2010)“…Michael addition of ethyl nitroacetate on α,β-unsaturated ketones followed by Nef oxidation under hydrolytic conditions yields γ-oxoacids instead of the…”
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Efficacy of a New Small-Molecule Inhibitor of Histone Deacetylase 6 (HDAC6) in Preclinical Models of B-Cell Lymphoma and Acute Myeloid Leukemia
Published in Blood (29-11-2018)“…Histone deacetylase 6 (HDAC6) is a protein modifier that is an increasingly attractive pharmacological target. Interestingly, the observation that the HDAC6…”
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In vitro and in vivo activity of a new small-molecule inhibitor of HDAC6 in mantle cell lymphoma
Published in Haematologica (Roma) (01-11-2018)“…Cancer origin and development is associated not only with genetic alterations, but also with the disturbance of epigenetic profiles.1 In this regard, the…”
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Double Insertion of Isocyanides into Dihydropyridines: Direct Access to Substituted Benzimidazolium Salts
Published in Angewandte Chemie International Edition (20-04-2007)“…Double agent: The insertion of two isocyanide molecules into the dihydropyridine ring in the presence of iodine results in the formation of a benzimidazole…”
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Isocyanide Addition to Pyridinium Salts. Efficient Entry into Substituted Nicotinonitrile Derivatives
Published in Organic letters (07-12-2006)“…The addition of isocyanides to pyridinium salts is studied. The process takes place efficiently when a carboxamido group is present in the 3 position of the…”
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Multicomponent Access to Functionalized Mesoionic Structures Based on TFAA Activation of Isocyanides: Novel Domino Reactions
Published in European Journal of Organic Chemistry (01-02-2009)“…The reactions of azines (isoquinolines, pyridine) with TFAA and isocyanides in a new domino process yield mesoionic acid fluorides with an imidazo[1,2‐a]azine…”
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Development and validation of a LC-MS assay for the quantification of ikh12 a novel anti-tumor candidate in rat plasma and tissues and its application in a pharmacokinetic study
Published in Biomedical chromatography (01-08-2015)“…IKH12 is a novel histone deacetylase 6 selective inhibitor. A rapid and sensitive liquid chromatography tandem mass spectrometry method was developed and…”
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Benzimidazolium Salts as Small, Nonpeptidic and BBB-Permeable Human Prolyl Oligopeptidase Inhibitors
Published in ChemMedChem (20-10-2008)“…Prolyl oligopeptidase (POP) is a cytosolic serine peptidase that hydrolyzes proline‐containing peptides at the carboxy terminus of proline residues. This…”
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Straightforward α-carbamoylation of NADH-like dihydropyridines and enol ethers
Published in Tetrahedron letters (11-10-2004)“…[Display omitted] The protonation of NADH-like dihydropyridines and cyclic enol ethers generates reactive cationic intermediates, which interact with…”
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