A5059149017- Cancer-related Molecular Pathways
- Fluorine in Organic Chemistry
- Receptor Mechanisms and Signaling
- Natural Compound Pharmacology Studies
- Computational Drug Discovery Methods
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Neuropeptides and Animal Physiology
- Neuroblastoma Research and Treatments
- Biological Activity of Diterpenoids and Biflavonoids
- Drug Transport and Resistance Mechanisms
- Radiopharmaceutical Chemistry and Applications
- Plant nutrient uptake and metabolism
- Cancer therapeutics and mechanisms
- Cannabis and Cannabinoid Research
- Monoclonal and Polyclonal Antibodies Research
- Chemical synthesis and alkaloids
- Inorganic Fluorides and Related Compounds
- HIV/AIDS Research and Interventions
- Marine Sponges and Natural Products
- Microtubule and mitosis dynamics
- Cell death mechanisms and regulation
- HIV/AIDS drug development and treatment
- Neuroscience and Neuropharmacology Research
- Radical Photochemical Reactions
Universidade do Porto
2015-2021
University of Liège
2018-2020
University of Coimbra
2018-2020
UCB Pharma (Belgium)
2020
Centro Interdisciplinar de Investigação Marinha e Ambiental
2019
Rede de Química e Tecnologia
2017-2018
John Wiley & Sons (United States)
2016
Despite a growing interest in CHF2 medicinal chemistry, there is lack of efficient methods for the insertion CHF18 F into druglike compounds. Herein described photoredox flow reaction 18 F-difluoromethylation N-heteroaromatics that are widely used chemistry. Following two-step synthesis new reagent, completed within two minutes and proceeds by C-H activation, circumventing need pre-functionalization substrate. The method operationally simple affords straightforward access to radiolabeled...
We recently reported a new method for the 18F-difluoromethylation of N-heteroaromatics positron emission tomography (PET) imaging. The involves synthesis 18F-difluoromethylating reagent, 2-[18F]((difluoromethyl)sulfonyl)benzo[d]thiazole, and flow photoredox 18F-difluoromethylation. For preclinical development human PET studies with radiotracers, automation process is mandatory, mostly to avoid radioprotection issues due use high amounts radioactivity ensure better reliability production....
Xanthone scaffold has been regarded as an attractive chemical tool in the search for bioactive molecules with antitumor activity, and particular two xanthone derivatives, 12-hydroxy-2,2-dimethyl-3,4-dihydro-2H,6H-pyrano [3,2-b]xanthen-6-one (4) 3,4-dimethoxy-9-oxo-9H-xanthene-1-carbaldehyde (5), were described a murine double minute 2 (MDM2)-p53 inhibitor TAp73 activator, respectively. The 5 was used starting point construction of library 3,4-dioxygenated xanthones bearing moieties MDM2-p53...
A series of thirteen xanthones 3–15 was prepared based on substitutional (appendage) diversity reactions. The structurally characterized their spectral data and HRMS, the structures xanthone derivatives 1, 7, 8 were determined by single-crystal X-ray diffraction. This series, along with an in-house aminated 16–33, tested for in-vitro antimicrobial activity against seven bacterial (including two multidrug-resistant) strains five fungal strains. 1-(Dibromomethyl)-3,4-dimethoxy-9H-xanthen-9-one...
P-glycoprotein (P-gp) plays a crucial role in the protection of susceptible organs, by significantly decreasing absorption/distribution harmful xenobiotics and, consequently, their toxicity. Therefore, P-gp has been proposed as potential antidotal pathway, when activated and/or induced. Knowing that xanthones are known to interact with P-gp, main goal was study induction or/and activation six new oxygenated (OX 1-6). Furthermore, Caco-2 cells against paraquat cytotoxicity also assessed. The...
Parkinson's Disease (PD) is a long-term neurodegenerative brain disorder that mainly affects the motor system. The causes are still unknown, and even though currently there no cure, several therapeutic options available to manage its symptoms. development of novel antiparkinsonian agents an understanding their proper optimal use are, indeed, highly demanding. For last decades, L-3,4-DihydrOxyPhenylAlanine or levodopa (L-DOPA) has been gold-standard therapy for symptomatic treatment...
The 18F-labeling of CF2H groups has been recently studied in radiopharmaceutical chemistry owing to the favorable nuclear and physical characteristics radioisotope 18F for positron emission tomography (PET). Following up on reported efficiency [18F]difluoromethyl benzothiazolyl-sulfone ([18F]1) as a 18F-difluoromethylating reagent, we investigated influence structurally-related heteroaryl-sulfones reactivity toward photoredox C–H 18F-difluoromethylation heteroarenes under continuous-flow...
Biofouling, which occurs when certain marine species attach and accumulate in artificial submerged structures, represents a serious economic environmental issue worldwide. The discovery of new non-toxic eco-friendly antifouling systems to control or prevent biofouling is, therefore, practical urgent need. In this work, the activity series 24 xanthones, with chemical similarities natural products, was exploited. Nine (
G-Protein coupled receptors (GPCRs) are involved in a myriad of pathways key for human physiology through the formation complexes with intracellular partners such as G-proteins and arrestins (Arrs). However, structural dynamical determinants these still largely unknown. Herein, we developed computational big-data pipeline that enables characterization GPCR no available structure. This was used to study well-known group catecholamine receptors, dopamine receptor (DXR) family its complexes,...
Abstract Despite a growing interest in CHF 2 medicinal chemistry, there is lack of efficient methods for the insertion 18 F into druglike compounds. Herein described photoredox flow reaction F‐difluoromethylation N‐heteroaromatics that are widely used chemistry. Following two‐step synthesis new reagent, completed within two minutes and proceeds by C−H activation, circumventing need pre‐functionalization substrate. The method operationally simple affords straightforward access to radiolabeled...
Typically, about 90% of drug candidates are N-containing, and an even higher amount O-containing. As a consequence, it is not surprising that alkylation arylation groups with nitrogen oxygen emerge as major reactions to obtain bioactive compounds.1 Xanthones class O-heterocycles characterized by dibenzo-γ-pyrone nucleus. This scaffold may be considered "privileged structure" able providing useful ligands for several types receptors and/or enzymes targets judicious structural modifications.2...
Open AccessExtended Abstract Strategies to Discover p53 Activators and a p73 Activator for Neuroblastoma † by Emília Sousa 1,2,*, Sara Gomes 3, Liliana Raimundo Joana Soares Loureiro Mariana Leão Helena Ramos Madalena Monteiro Petr Chlapek 4, Renata Veselská Agostinho Lemos 1,2, Moreira Pinto 1,2 Lucilia Saraiva 3 1 Department of Chemical Sciences, Laboratory Organic Medicinal Chemistry, Faculty Pharmacy, University Porto,4050-313 Porto, Portugal 2 CIIMAR—Interdisciplinary Centre Marine...
TAp73 is a key tumour suppressor protein, regulating the transcription of unique and shared p53 target genes with crucial roles in tumorigenesis therapeutic response. As such, tumours impaired signalling, like neuroblastoma (NBL), activation represents an encouraging strategy, alternative to activation, suppress growth chemoresistance [1]. Actually, NBL one most common childhood solid cancers but despite available treatments, high-risk patients are still characterized by low survival rates,...