A5015747605- Radiopharmaceutical Chemistry and Applications
- Boron Compounds in Chemistry
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Boron and Carbon Nanomaterials Research
- Click Chemistry and Applications
- Crystallography and molecular interactions
- RNA Interference and Gene Delivery
- Organoboron and organosilicon chemistry
- Monoclonal and Polyclonal Antibodies Research
- Fluorine in Organic Chemistry
- Neonatal Health and Biochemistry
- Cell death mechanisms and regulation
- Glutathione Transferases and Polymorphisms
- Trypanosoma species research and implications
- Educational Research and Science Teaching
- Genomics, phytochemicals, and oxidative stress
- Analytical Chemistry and Sensors
- Hispanic-African Historical Relations
- Autophagy in Disease and Therapy
- Research on Leishmaniasis Studies
- Photodynamic Therapy Research Studies
- Sulfur-Based Synthesis Techniques
- Synthesis of heterocyclic compounds
- Supramolecular Chemistry and Complexes
Universidad de la República
2014-2025
Institut de Ciència de Materials de Barcelona
2017-2020
Consejo Superior de Investigaciones Científicas
2020
Universidad La República
2014-2018
Instituto de Química Orgánica General
2018
Universidad de Montevideo
2018
Abstract New 1,7‐ closo ‐carboranylanilinoquinazoline hybrids have been identified as EGFR inhibitors, one of them with higher affinity than the parent compound erlotinib. The comparative docking analysis compounds bearing bioisoster‐substructures, demonstrated relevance 3D aromatic‐boron‐rich moiety for interacting into ATP binding region. capability to accumulate in glioma cells, ability cross blood–brain barrier and stability on simulated biological conditions, render these molecules lead...
Abstract The reported new anilinoquinazoline‐icosahedral borane hybrids have been evaluated as glioma targeting for potential use in cancer therapy. Their anti ‐glioma activity depends on hybrids’ lipophilicity; the most powerful compound against cells, a 1,7‐ closo ‐derivative, displayed at least 3.3 times higher than parent drug erlotinib. According to cytotoxic effects normal glia were selective epidermal growth factor receptor (EGFR)‐overexpressed tumor cells. These boron carriers could...
Abstract About 95 % of people diagnosed with glioblastoma die within five years. Glioblastoma is the most aggressive central nervous system tumour. It necessary to make progress in treatment so that advanced chemotherapy drugs or radiation therapy or, ideally, two‐in‐one hybrid systems should be implemented. Tyrosine kinase receptors–inhibitors and boron neutron capture (BNCT), together, could provide a therapeutic strategy. In this work, sunitinib decorated‐carborane hybrids were prepared...
Background/Objectives: Boron neutron capture therapy (BNCT) is a promising approach for selectively targeting and destroying malignant cells using 10B isotopes. A significant challenge in BNCT lies the development of efficient boron delivery systems that ensure adequate accumulation within tumor cells. This study aims to synthesize, characterize, evaluate COSAN-functionalized nanoparticles (NP@I-COSAN) as potential carrier BNCT. Methods: Hybrid were synthesized by conjugating monoiodinated...
One of the driving forces carcinogenesis in humans is aberrant activation receptors; consequently, one most promising mechanisms for cancer treatment receptor inhibition by chemotherapy. Although a variety cancers are initially susceptible to chemotherapy, they eventually develop multi-drug resistance. Anti-tumor agents overcoming resistance and acting through two or more ways offer greater therapeutic benefits over single-mechanism entities. In this study, we report on new family...
Favipiravir is an important selective antiviral against RNA-based viruses, and currently, it being repurposed as a potential drug for the treatment of COVID-19. This type chemical system presents different carboxamide-rotameric hydroxyl-tautomeric states, which could be essential interpreting its activity. Herein, tautomeric 3-hydroxypyrazine/3-pyrazinone pair favipiravir 6-substituted analogues, 6-Cl, 6-Br, 6-I, 6-H, were fully investigated in solution solid state through...
Since Locher proposed the concept of boron neutron capture therapy (BNCT) in 1936, it has become a great challenge field medicinal chemistry. The dare been to obtain boron-containing compounds that selectively accumulate organ be irradiated. Polyhedral clusters (PBC) have considered attractive moieties for development BNCT-agents due their large contribution per molecule. Various issues arose first efforts develop PBC during 1940-1950s prevented application BNCT clinical trials, such as lack...
Malignant gliomas are the most common malignant and aggressive primary brain tumors in adults, prognosis being—especially for glioblastomas—extremely poor. There no effective treatments yet. However, tyrosine kinase receptor (TKR) inhibitors boron neutron capture therapy (BNCT), together, have been proposed as future therapeutic strategies. In this sense our ongoing project of developing new anti-glioblastoma drugs, we identified a sunitinib-carborane hybrid agent, 1, with both vitro...
Glioblastoma (GBM), as the most central nervous system (CNS) intractable disease, has spoiled millions of lives due to its high mortality. Even though several efforts have been made, existing treatments had limited success. In this sense, we studied a lead compound, boron-rich selective epidermal growth factor receptor (EGFR)-inhibitor hybrid 1, potential drug for GBM treatment. For end, analyzed in vitro activity 1 glioma/primary astrocytes coculture, studying cellular death types triggered...
A novel efficient one-step synthetic strategy for the preparation of antiviral favipiravir from with available 3-hydroxy-2-pyrazinecarboxamide and Selectfluor® was developed, use an IL being essential.
Background: Carboranylanilinoquinazoline-hybrids, developed for boron neutron capture therapy, have demonstrated cytotoxicity against murine-glioma cells with EGFR-inhibition ability. In addition, their adequate aqueous/metabolic stabilities and ability to cross blood–brain barrier make them good leads as become antiglioma drugs. Aim: Analyze drug-like properties of representative carboranylanilinoquinazolines. Materials & methods: To expand carboranylanilinoquinazolines therapeutic...
Pretargeted imaging is shown to be an attractive strategy overcome disadvantages associated with traditional radioimmunoconjugates.
The current pharmacological Chagas disease treatments, using Nifurtimox or Benznidazole, show limited therapeutic results and are associated with potential side effects, like mutagenicity. Using random screening we have identified new chemotypes that were able to inhibit relevant targets of the Trypanosoma cruzi. We found 3H-[1,2]dithioles ability cruzi triosephosphate isomerase (TcTIM). Herein, studied structural modifications this chemotype analyze influence volume, lipophilicity...
Cancer chemoprevention involves the carcinogenic process prevention, delay or reverse by administration of chemopreventive agents, which are able to suppress block carcinogen metabolic activation/formation. The increased activity phase II detoxification enzymes such as quinone-reductase (QR) and glutation-S-transferase (GST) correlates with protection against chemically-induced carcinogenesis. It has been shown that synthetic chalcones 3H-[1,2]-dithiole-3-thiones promote expression genes...
The photophysical properties of favipiravir and its 6-halogenated analogues are presented, the origin fluorescence was interpreted as a function 3-OH tautomerism.
An EGFR inhibitor that incorporates closo-carborane has been shown to have higher affinity than erlotinib. The comparative docking analysis with compounds bearing bioisoster substructures demonstrated the relevance of 3D aromatic boron-rich moiety for interacting into ATP binding region. capability accumulate in glioma cells, ability cross blood–brain barrier and stability under simulated biological conditions render these molecules as lead further structural modifications obtain dual action...
Nuestro primer curso de Química orgánica, donde se presentan los principales grupos funcionales, sus propiedades fisicoquímicas y síntesis, poseía un contenido estrictamente teórico. Por este motivo, en muchas temáticas, especialmente físicas ácido-base compuestos orgánicos reacciones reconocimientos funcionales estudiantes no conseguían traspasar la barrera del aprendizaje significativo. eso, como forma complementar fortalecer instancia adquisición conocimientos, decidimos implementar una...