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Synthesis of novel hybrid quinolino[4,3-b][1,5]naphthyridines and quinolino[4,3-b][1,5]naphthyridin-6(5H)-one derivatives and biological evaluation as topoisomerase I inhibitors and antiproliferatives
(Elsevier, 2020-04-03)
The topoisomerase I enzymatic inhibition of hybrid quinolino [4,3-b] (Siegel et al., 2013; Antony et al., 2003) [1,5]naphthyridines and quinolino [4,3-b] (Siegel et al., 2013; Antony et al., 2003) [1,5]naphthyridin-6(5H)-ones ...
Novel phosphine sulphide gold(I) complexes: topoisomerase I inhibitors and antiproliferative agents
(RSC, 2020-05-20)
This work describes the synthesis of the gold(I) complexes of phosphine sulphides. The formation of these new derivatives has been confirmed by X-ray crystallography. The coordination of gold(I) with the sulphur atom of ...
Probing α‐Amino Aldehydes as Weakly Acidic Pronucleophiles: Direct Access to Quaternary α‐Amino Aldehydes by an Enantioselective Michael Addition Catalyzed by Brønsted Bases
(Wiley, 2020-10-09)
The high tendency of α-amino aldehydes to undergo 1,2-additions and their relatively low stability under basic conditions have largely prevented their use as pronucleophiles in the realm of asymmetric catalysis, particularly ...
Phosphine-catalysed transformations of ortho- and para-quinone methides
(RSC, 2023)
Organocatalytic methodologies for the derivatization of o-QM, p-QM and the analogous aza-QM have been recently developed and involve different catalytic systems such as phosphoric acids, thioureas, squaramides, NHC carbenes ...
Design, synthesis and cytotoxic evaluation of diphenyl(quinolin-8-yl)phosphine oxides
(Elsevier, 2021-04)
A new strategy is reported for the synthesis of quinolinylphosphine oxides via the Povarov reaction between phosphorous aldimines and acetylenes. Moreover, these compounds were studied for in vitro cytotoxicity on a human ...
Synthesis, biological and computational evaluation of novel cyanomethyl vinyl ether derivatives
(Frontiers Media, 2024)
This work explores the biological evaluation of novel cyanomethyl vinyl ether derivatives as antiproliferative agents. Tubulin, crucial to microtubule structure and function, is a target for cancer therapies. In vitro ...
Dehydration of alcohols catalyzed by copper(ii) sulfate: type II dyotropic reactions and stepwise mechanisms
(RSC, 2024)
Dehydration of alcohols in the presence of copper(II) sulfate has been analyzed computationally. Density functional theory (DFT) calculations on selected alcohols indicate that this reaction can take place via two possible ...
β2, 2-Amino Acid N-Carboxyanhydrides Relying on Sequential Enantioselective C(4)-Functionalization of Pyrrolidin-2,3-diones and Regioselective Baeyer–Villiger Oxidation
(Wiley, 2017-02-28)
A catalytic enantioselective entry to β2, 2-amino acids enabling their direct coupling with nucleophiles is described. The approach is based upon an effective bifunctional Brønsted base catalyzed construction of a quaternary ...
Diastereoselective ZnCl2-Mediated Joullié–Ugi Three-Component Reaction for the Preparation of Phosphorylated N-Acylaziridines from 2H-Azirines
(MDPI, 2024-02-27)
We disclose a direct approach to the diastereoselective synthesis of phosphorus substituted N-acylaziridines based on a one-pot ZnCl2-catalyzed Joullié–Ugi three-component reaction of phosphorylated 2H-azirines, carboxylic ...
Extended Enolates: Versatile Intermediates for Asymmetric C-H Functionalization via Noncovalent Catalysis
(Wiley, 2021)
Catalyst-controlled functionalization of unmodified carbonyl compounds is a relevant operation in organic synthesis, especially when high levels of site- and stereo-selectivity can be attained. This objective is now within ...