Luiz Antônio Dutra
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View article: Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε
Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε Open
Vaccinia-related kinase 1 (VRK1) and the δ and ε isoforms of casein kinase 1 (CK1) are linked to various disease-relevant pathways. However, the lack of tool compounds for these kinases has significantly hampered our understanding of their…
View article: Novel dihydropteridinone derivatives as potent and selective inhibitors of the understudied human vaccinia-related kinase 1 (VRK1)
Novel dihydropteridinone derivatives as potent and selective inhibitors of the understudied human vaccinia-related kinase 1 (VRK1) Open
The human Vaccinia-Related Kinase 1 (VRK1) is highly expressed in various tumor types and plays important roles in cell proliferation and the maintenance of genome integrity. While prior genetic studies indicate that VRK1 inhibition offers…
View article: Twenty-five years of natural products research in NuBBE
Twenty-five years of natural products research in NuBBE Open
The richness of Brazilian biodiversity translates into a valuable collection of molecules with biological properties that range from ecological functions to pharmacological properties. For over 25 years, the Nucleus of Bioassays, Biosynthe…
View article: Homology Modeling of Alpha-Glucosidase from Candida albicans: Sequence Analysis and Structural Validation Studies in silico
Homology Modeling of Alpha-Glucosidase from Candida albicans: Sequence Analysis and Structural Validation Studies in silico Open
The alpha-glucosidase enzyme of Candida albicans plays a vital role in the pathogenesis of candidiasis, a serious fatal disease in immune-compromised patients. The unavailability of the threedimensional crystallographic structure of this e…
View article: Discovery of (E)-4-styrylphenoxy-propanamide: A dual PPARα/γ partial agonist that regulates high-density lipoprotein-cholesterol levels, modulates adipogenesis, and improves glucose tolerance in diet-induced obese mice
Discovery of (E)-4-styrylphenoxy-propanamide: A dual PPARα/γ partial agonist that regulates high-density lipoprotein-cholesterol levels, modulates adipogenesis, and improves glucose tolerance in diet-induced obese mice Open
View article: Identification of a Prenyl Chalcone as a Competitive Lipoxygenase Inhibitor: Screening, Biochemical Evaluation and Molecular Modeling Studies
Identification of a Prenyl Chalcone as a Competitive Lipoxygenase Inhibitor: Screening, Biochemical Evaluation and Molecular Modeling Studies Open
Cyclooxygenase (COX) and lipoxygenase (LOX) are key targets for the development of new anti-inflammatory agents. LOX, which is involved in the biosynthesis of mediators in inflammation and allergic reactions, was selected for a biochemical…
View article: Antifungal Activity of 2′-Hydroxychalcone Loaded in Nanoemulsion Against <i>Paracoccidioides</i> Spp.
Antifungal Activity of 2′-Hydroxychalcone Loaded in Nanoemulsion Against <i>Paracoccidioides</i> Spp. Open
Aim: This study aimed to evaluate the activity of 2'-hydroxychalcone-loaded in nanoemulsion (NLS + 2'chalc), the cytotoxic effect and toxicity against Paracoccidioides brasiliensis and Paracoccidioides lutzii using a z…
View article: Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2
Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2 Open
Vaccinia-related kinases 1 and 2 (VRK1 and VRK2) are human Ser/Thr protein kinases associated with increased cell division and neurological disorders. Nevertheless, the cellular functions of these proteins are not fully understood. Despite…
View article: Development of Pyridine-Based Inhibitors for the Human Vaccinia-Related Kinases 1 and 2
Development of Pyridine-Based Inhibitors for the Human Vaccinia-Related Kinases 1 and 2 Open
Vaccinia-related kinases 1 and 2 (VRK1 and VRK2) are human Ser/Thr protein kinases associated with increased cell division and neurological disorders. Nevertheless, the cellular functions of these proteins are not fully understood. Despite…
View article: Development of Pyridine-Based Inhibitors for the Human Vaccinia-Related Kinases 1 and 2
Development of Pyridine-Based Inhibitors for the Human Vaccinia-Related Kinases 1 and 2 Open
Vaccinia-related kinases 1 and 2 (VRK1 and VRK2) are human Ser/Thr protein kinases associated with increased cell division and neurological disorders. Nevertheless, the cellular functions of these proteins are not fully understood. Despit…
View article: Thermal study of chalcones
Thermal study of chalcones Open
View article: Planejamento, síntese e avaliação farmacológica de novos compostos híbridos derivados de resveratrol e bezafibrato úteis ao tratamento da dislipidemia
Planejamento, síntese e avaliação farmacológica de novos compostos híbridos derivados de resveratrol e bezafibrato úteis ao tratamento da dislipidemia Open
View article: Chemical constituents from Casearia spp. (Flacourtiaceae/Salicaceae sensu lato )
Chemical constituents from Casearia spp. (Flacourtiaceae/Salicaceae sensu lato ) Open
View article: Dietary Compound Resveratrol Is a Pan-BET Bromodomain Inhibitor
Dietary Compound Resveratrol Is a Pan-BET Bromodomain Inhibitor Open
The chemopreventive and anticancer effects of resveratrol (RSV) are widely reported in the literature. Specifically, mechanisms involving epigenetic regulation are promising targets to regulate tumor development. Bromodomains act as epigen…
View article: Síntese de (E)-dimetoxi-estilbenos com atividade preventiva a aterosclerose in vitro
Síntese de (E)-dimetoxi-estilbenos com atividade preventiva a aterosclerose in vitro Open
Introducao: A aterosclerose e uma doenca inflamatoria cronica causada por alteracoes no metabolismo lipidico com crescente acumulo de LDL-C na camada intima das arterias. Macrofagos fagocitam LDL-C e transformam-se em celulas espumosas que…
View article: In vivo antileishmanial activity and histopathological evaluation in Leishmania infantum infected hamsters after treatment with a furoxan derivative
In vivo antileishmanial activity and histopathological evaluation in Leishmania infantum infected hamsters after treatment with a furoxan derivative Open
View article: Synthesis, antiplatelet and antithrombotic activities of resveratrol derivatives with NO-donor properties
Synthesis, antiplatelet and antithrombotic activities of resveratrol derivatives with NO-donor properties Open
View article: Corrigendum to “The 2′,4′-dihydroxychalcone could be explored to develop new inhibitors against the glycerol-3-phosphate dehydrogenase from Leishmania species” [Bioorg. Med. Chem. Lett. 25 (2015) 3564–3568]
Corrigendum to “The 2′,4′-dihydroxychalcone could be explored to develop new inhibitors against the glycerol-3-phosphate dehydrogenase from Leishmania species” [Bioorg. Med. Chem. Lett. 25 (2015) 3564–3568] Open
View article: Synthesis and evaluation of the thermal behavior of flavonoids
Synthesis and evaluation of the thermal behavior of flavonoids Open
View article: The Paradigma of the Interference in Assays for Natural Products
The Paradigma of the Interference in Assays for Natural Products Open