A5047401565- Biochemical and Molecular Research
- HIV/AIDS drug development and treatment
- Chemical Synthesis and Analysis
- Pneumocystis jirovecii pneumonia detection and treatment
- Fluorine in Organic Chemistry
- Quinazolinone synthesis and applications
- Chronic Lymphocytic Leukemia Research
- Synthesis and Characterization of Heterocyclic Compounds
- Chemical Synthesis and Reactions
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Carbohydrate Chemistry and Synthesis
- Synthesis and Catalytic Reactions
- Prostate Cancer Treatment and Research
- Lipid Membrane Structure and Behavior
- Axial and Atropisomeric Chirality Synthesis
- Radiopharmaceutical Chemistry and Applications
- Cancer therapeutics and mechanisms
- Urinary Tract Infections Management
- Hepatitis C virus research
- Phenothiazines and Benzothiazines Synthesis and Activities
- Organoboron and organosilicon chemistry
- Asymmetric Synthesis and Catalysis
- Mass Spectrometry Techniques and Applications
- Sphingolipid Metabolism and Signaling
Cardiff University
2014-2024
Edwards (United Kingdom)
2018-2024
King Edward VII Hospital
2017
University of Southern California
2011-2014
Emory University
2008
Prostate cancer (PC) is one of the major causes male death worldwide and development new more potent anti-PC compounds a constant requirement. Among current treatments, (R)-bicalutamide enzalutamide are non-steroidal androgen receptor antagonist drugs approved also in case castration-resistant forms. Both these present moderate antiproliferative activity their use limited due to resistant mutants biological target. Insertion fluorinated perfluorinated groups biologically active trend...
The first copper-catalysed diastereoselective synthesis of P-chiral phosphoramidate prodrugs (ProTides) is reported. This procedure allows the diastereomeric-enriched mixtures ProTides. Application this methodology to asymmetric phosphorylation purine and pyrimidine nucleoside analogues presented.
Disease-modifying osteoarthritis drugs (DMOADs) are a new therapeutic class for (OA) prevention or inhibition of the disease development. Unfortunately, none DMOADs have been clinically approved due to their poor performances in clinical trials. The joint environment has played role this process by limiting amount drug effectively delivered as well time that stays within space. current study aimed improve delivery into cartilage tissue increasing uptake and retention tissue. Licofelone was...
We report the synthesis of a family D- and L-furano-D-apionucleosides, their 3'-deoxy, as well 2',3'-dideoxy analogues with thymine adenine nucleobases. Single carbon homologation 1,2-O-isopropylidene-D-glycero-tetrafuranos-3-ulose (15) optimized glycosylation conditions involving microwave irradiation were key to successful target compounds. While all nucleosides failed show significant antiviral activity, we demonstrated that triphosphate 2',3'-deoxy-D-apio-D-furanoadenosine (1), in...
The ProTide (pronucleotide) approach is a prodrug strategy elaborated to deliver nucleoside monophosphate into the cell, circumventing first and inefficient rate-limiting phosphorylation step of nucleosides improving cellular penetration nucleotides. phosphate phosphoramidate consisting an amino acid ester promoiety linked via P-N bond aryl phosphate. Such prodrugs have increased lipophilicity thus are capable altering cell tissue distribution. technology was successfully extensively applied...
Abstract A series of tritylated and dimethoxytritylated analogues selected pyrimidine purine nucleosides were synthesized evaluated for their in vitro inhibitory activity against two important members the genus Flavivirus Flaviviridae family, yellow fever (YFV) dengue viruses (DENV). Among all compounds tested, 5′‐O‐tritylated 5′‐O‐dimethoxytritylated 5‐fluorouridine derivatives exerted potency YFV. Interestingly analogues, 5′O, N‐bis‐tritylated fludarabine derivative revealed strong DENV at...
Following a drug repurposing approach, we aimed to investigate and compare the antibacterial antibiofilm activities of different classes phosphate prodrugs (HepDirect, cycloSal, SATE mix SATE) antiviral anticancer FDA-approved nucleoside drugs [zidovudine (AZT), floxouridine (FUDR) gemcitabine (GEM)] against variety pathogenic Gram-positive -negative bacteria.Ten were synthesized screened for activity seven Gram-negative two isolates fully susceptible traditional antibiotics, alongside six...
Amongst drug resistant Gram-positive bacteria,
The direct preparation of tetrabutylammonium trifluoroborates from boronic acids without using HF or the corresponding potassium salt is described. method highly efficient for aromatic and aliphatic acids. This protocol, however, was less that were sensitive to protiodeboronation.
ProTides comprise an important class of prodrugs currently marketed and developed as antiviral anticancer therapies. The ProTide technology employs phosphate masking groups capable providing more favorable druglike properties intracellular activation mechanism for enzyme-mediated release a nucleoside monophosphate. Herein, we describe the application phosphoramidate chemistry to 1,3,4-O-acetylated N-acetylmannosamine (Ac3ManNAc) deliver ManNAc-6-phosphate (ManNAc-6-P), critical intermediate...
Aryloxy phosphoroamidate triesters, known as ProTides, are a class of prodrugs developed to enhance the physicochemical and pharmacological properties therapeutic nucleosides. This approach has been extensively investigated in antiviral anticancer areas leading three on market several others clinical stage. In this article we have prepared PS analogues ProTides that reached clinic agents. These novel were tested for their capacity enzymatic activation cytotoxic against panel solid liquid...