A5043229188- Bioactive Compounds and Antitumor Agents
- Catalytic C–H Functionalization Methods
- Synthesis and Biological Evaluation
- Chemical synthesis and alkaloids
- Cancer therapeutics and mechanisms
- Organic Chemistry Cycloaddition Reactions
- Sulfur-Based Synthesis Techniques
- Morinda citrifolia extract uses
- Catalytic Cross-Coupling Reactions
- Cyclopropane Reaction Mechanisms
- Quinazolinone synthesis and applications
- Trypanosoma species research and implications
- HIV/AIDS drug development and treatment
- Phytochemical compounds biological activities
- Photodynamic Therapy Research Studies
- Multicomponent Synthesis of Heterocycles
- Antimicrobial agents and applications
- Advanced Drug Delivery Systems
- Asymmetric Hydrogenation and Catalysis
- Women's cancer prevention and management
- Skin Protection and Aging
- Porphyrin Metabolism and Disorders
- Curcumin's Biomedical Applications
- Law, Ethics, and AI Impact
- Synthesis and Reactivity of Heterocycles
Universidade Federal de Santa Maria
2020-2025
Universidade de São Paulo
2013-2019
Universidade de Ribeirão Preto
2013-2019
University of Göttingen
2018
meta-Selective C-H alkylations of bioactive purine derivatives were accomplished by versatile ruthenium catalysis. Thus, the arene-ligand-free complex [Ru(OAc)2 (PPh3 )2 ] enabled remote functionalizations with ample scope and excellent levels chemo- positional selectivities. Detailed experimental computational mechanistic studies provided strong support for a facile activation within ruthenium(II/III) manifold.
The 1,4-naphthoquinones, important members of the family quinones are used as both crude extracts and compound manipulated by pharmaceutical industry. They have gained great emphasis presenting different pharmacological properties antibacterial, antiviral, antiprotozoal anthelmintic, has antitumor activity. Our aim was to evaluate cytotoxicity, hemolytic activity in vivo acute toxicity three derivatives 2-hydroxy-1,4-naphthoquinones. cell viability vitro against RAW Cell Line displayed IC50...
We developed poly-ε-caprolactone (PCL)-based nanoparticles containing D-α-tocopherol polyethylene glycol-1000 succinate (TPGS) or Poloxamer 407 as stabilizers to efficiently encapsulate genistein (GN). Two formulations, referred PNTPGS and PNPol, were prepared using nanoprecipitation. They characterized by size PDI distribution, zeta potential, nanoparticle tracking analysis (NTA), GN association (AE%), infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC). PNTPGS-GN...
Heterocycle cores are widely used in medicinal chemistry for developing bioactive compounds. In this scenario, using cheap and accessible starting material to build these heterocycles is desirable obtain new drug candidates cost-efficient processes. One easily source of amino acids. Usually, compounds employed peptide synthesis, but their use building heterocycle frameworks presents another appealing opportunity. Therefore, review highlights the application histidine tryptophan, two...
A concise strategy for the synthesis of 2,3-substituted furo[2,3-b]pyridines is described. Mild, metal-free conditions were successfully applied to produce a range 2-(alkyl or aryl)-3-ethylcarboxylate-furo[2,3-b]pyridines in yields 50–91%. Then, chemical reactivity this heterocyclic framework was explored develop straightforward methods its functionalization. The pyridine moiety by C–H amination and borylation reactions, although fluorination radical arylation processes not as efficient. In...
Neglected tropical diseases remain among the most critical public health concerns in Africa and South America. The drug treatments for these are limited, which invariably leads to fatal cases. Hence, there is an urgent need new antitrypanosomal drugs. To address this issue, a large number of diverse heterocyclic compounds were prepared. Straightforward synthetic approaches tolerated pre-functionalized structures, giving rise structurally set analogs. We report on 57 with selective activity...
Background: Lead-like drugs, which present molecular weight (MW) < 300 Da, occupy an important space in the pharmaceutical area. Most of these small molecules have ring systems, are for their physicochemical properties and biological activity. Previous studies evaluated systems historic drugs or drug candidates clinical trials. Objective: The purpose this work was to analyze focusing on group with MW obtain specific insights. Methods: lead-like (n = 219) were obtained from previous...
Lapachol is a natural naphthoquinone with range of biological effects, including anticancer activity. Microbial transformations lapachol can lead to the formation new biologically active compounds. In addition, fungi produce secondary metabolites that are also important for drug discovery. The goal this study was evaluate ability filamentous biotransform into compounds and identify produced in presence lapachol. Seven out nine strains tested exhibited or biodegrade bioactive derivatives...
Introdução: Os anticorpos monoclonais (mAb) são alternativa terapêutica importante no tratamento do câncer. Porém, o acesso a essa terapia é desigual entre países com diferentes rendas. Objetivo: Comparar os fármacos mAb aprovados para uso contra câncer nos EUA Brasil e discutir, por meio mecanismo de ação, alternativas terapêuticas disponíveis. Método: A lista pelo FDA foi coletada publicação prévia complementada dados presentes site dessa agência, assim como data aprovação indicações...
Background: Although evaluating in vitro biological activity is an important part of the drug discovery process, few publications discuss ideal inhibitory these tests. Objective: To analyze data from antiviral drugs to establish parameters that could increase success developing new candidates. Methods: Information tests for each medicine was obtained Thomson Reuters Integrity platform approved by FDA between 1963 and 2020 (35 years). The collected three references using same determination...
The development of new bioactive compounds is necessary to address diseases that have few or no treatments. Diversity-oriented synthesis (DOS) helps in identifying hits and lead compounds, based on the prototypes with known biological activity. Natural products are good sources can be used design drugs. recently described carbazole alkaloid Clauraila A (Fig. 1), isolated from Clausena harmandiana, a typical example prototype compound allows researchers study structure-activity relationships...
Abstract The title compounds (III) are obtained by the underexplored epoxide‐opening reaction of 2,3‐epoxy‐1,4‐naphthoquinone using aniline derivatives as nucleophiles.