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Hitting a Moving Target: Simulation and Crystallography Study of ATAD2 Bromodomain Blockers
(ACS Publications, 2020-06-30)Small molecule ligand binding to the ATAD2 bromodomain is investigated here through the synergistic combination of molecular dynamics and protein crystallography. A previously unexplored conformation of the binding pocket ... -
Catalyzed Methods to Synthesize Pyrimidine and Related Heterocyclic Compounds
(MDPI, 2023-01-12)This review covers articles published in the period from 2010 to mid-2022 on synthetic advances in the formation of pyrimidine and related heterocyclic compounds. Special emphasis has been given to the different types ... -
Synthesis of (-)- and (+)-Gummiferol via Asymmetric Synthesis of Glycidic Amides.
(Thieme, 2016)An efficient synthesis of the natural product (–)-gummiferol is achieved according to a novel asymmetric methodology of epoxide formation based on a new class of chiral sulfonium salts. This new methodology allows the rapid ... -
Indolenine-Based Derivatives as Customizable Two-Photon Fluorescent Probes for pH Bioimaging in Living Cells
(American Chemical Society, 2020)Novel pH probes based on 2-(6-methoxynaphthalen-2-yl)-3,3-dimethyl3H-indole have been synthesized and characterized. These compounds display excellent “off−on” fluorescence responses to acidic pH especially under two-photon ... -
Nickel-Catalyzed Enantioselective Electrochemical Reductive Cross-Coupling of Aryl Aziridines with Alkenyl Bromides
(ACS, 2023-03-07)An electrochemically driven nickel-catalyzed enantioselective reductive cross-coupling of aryl aziridines with alkenyl bromides has been developed, affording enantioenriched β-aryl homoallylic amines with excellent ... -
Bengamide Analogues Show a Potent Antitumor Activity against Colon Cancer Cells: A Preliminary Study
(2020-05-02)The limited success and side effects of the current chemotherapeutic strategies against colorectal cancer (CRC), the third most common cancer worldwide, demand an assay with new drugs. The prominent antitumor activities ... -
Exploring the Antiangiogenic Potential of Solomonamide A Bioactive Precursors: In Vitro and In Vivo Evidences of the Inhibitory Activity of Solo F-OH During Angiogenesis
(2019-04-15)Marine sponges are a prolific source of bioactive compounds. In this work, the putative antiangiogenic potential of a series of synthetic precursors of Solomonamide A, a cyclic peptide isolated from a marine sponge, was ... -
Dual Nickel/Photoredox-Catalyzed Asymmetric Carbosulfonylation of Alkenes
(ACS, 2023-05-30)An asymmetric three-component carbosulfonylation of alkenes is presented here. The reaction, involving the simultaneous formation of a C–C and a C–S bond across the π-system, uses a dual nickel/photoredox catalytic system ... -
Energy-Transfer Sensitization of BODIPY Fluorescence in a Dyad with a Two-Photon Absorbing Antenna Chromophore
(Elsevier, 2023)A bichromophoric dyad composed of a Prodan-derived moiety and a BODIPY dye was prepared, photophysically characterized, and tested for multiphoton fluorescence microscopy of N13 microglial cells. The dyad shows highly ... -
Synthesis and Antitumor Activity Evaluation of Compounds Based on Toluquinol
(MDPI, 2019-08-23)Encouraged by the promising antitumoral, antiangiogenic, and antilymphangiogenic properties of toluquinol, a set of analogues of this natural product of marine origin was synthesized to explore and evaluate the effects of ... -
Identification of an Antigenic Determinant of Clavulanic Acid Responsible for IgE‐mediated Reactions
(John Wiley and Sons Ltd., 2019)Background: Selective reactions to clavulanic acid (CLV) account for around 30% of immediate reactions after administration of amoxicillin‐CLV. Currently, no immunoas‐ say is available for detecting specific IgE to CLV, ... -
Extended Alkenyl and Alkynyl Benzotriazoles with enhanced Two‐Photon Absorption properties as a promising alternative to Benzothiadiazoles
(Wiley-VCH Verlag GmbH & Co, 2019)A series of donor–p–acceptor–p–donor (D-p-A-p-D) benzoazole dyes with 2H-benzo[d][1,2,3]triazole or BTDcores have been prepared and their photophysical proper-ties characterized. The properties of these compounds dis-play ... -
Synthesis of Amino Terminal Clicked dendrimers. Approaches to the application as a biomarker
(ACS Publications, 2019)Herein, we present an easy and efficient synthesis of amino terminal dendrons, combining protection/deprotection reactions with copper-catalyzed azide alkyne cycloaddition in a convergent way. This new approach affords ... -
A Turn-On Two-Photon Fluorescent Probe for Detecting Lysosomal Hydroxyl Radicals in Living Cells.
(Elsevier, 2019)The detection of reactive oxygen species (ROS) in biological systems and its imaging is of great importance. Among them, the hydroxyl radical (radical dotOH) stands out as one of the most reactive, playing an important ... -
Rapid amplitude-modulation of a diarylethene photoswitch: En route to contrast-enhanced fluorescence imaging
(The Royal Society of Chemistry, 2021)A water soluble diarylethene (DAE) derivative that displays exceptionally intense fluorescence from the colorless open form has been synthesized and characterized using UV/vis spectroscopy and fluorescence microscopy. ... -
The Role of Benzylpenicilloyl Epimers in Specific IgE Recognition
(Frontiers, 2021)The high prevalence of allergy to β-lactam antibiotics is a worldwide issue. Accuracy of diagnostic methods is important to prove tolerance or allergy, with skin test considered the best validated in vivo method for ... -
Toward Two-Photon Absorbing Dyes with Unusually Potentiated Nonlinear Fluorescence Response
(American Chemical Society, 2020)The combination of two two-photon-induced processes in a Förster resonance energy transfer (FRET)-operatedphotochromic fluorene-dithienylethene dyad lays the foundation for the observation of a quartic dependence of the ... -
Synthesis of (-)-cannabidiol (CBD),(-)-Δ9- and(-)--Δ8-tetrahydrocannabinols, encapsulation of CBD with nanoparticles for controlled delivery and biological evaluation
(Wiley, 2024-12)Cannabidiol (CBD) is garnering increasing interest due to its significant biological activity. This natural compound is one of the major cannabinoids in Cannabis sativa L. In this work, we describe the encapsulation of CBD ... -
An array of bengamide E analogues modified at the terminal olefinic position: Synthesis and antimor properties.
(Chemistry Europe · European Chemical Societies Publishing, 2013-03-19)Based on our previously described synthetic strategy for bengamide E, a natural product of marine origin with antitumor activity, a small library of analogues modified at the terminal olefinic position was generated with ... -
An olefin metathesis approach towards the solomonamides.
(Elsevier, 2016)A new synthetic strategy directed towards the solomonamides, a novel class of cyclopeptides of marine origin, has been developed utilizing an olefin metathesis reaction to form the [15]-membered ring contained in these ...