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The Intramolecular Povarov Tool in the Construction of Fused Nitrogen-Containing Heterocycles
(Springer, 2023-06)
Nitrogen heterocycles are part of the structure of natural products and agents with
important biological activity, such as antiviral, antibiotic, and antitumor drugs. For
this reason, heterocyclic compounds are one of ...
Efficient AntiMycolata Agents by Increasing the Lipophilicity of Known Antibiotics through Multicomponent Reactions
(MDPI, 2023-01-03)
New antibiotic agents were prepared using Povarov and Ugi multicomponent reactions upon the known drugs sulfadoxine and dapsone. The prepared derivatives, with increased lipophilicity, showed improved efficiency against ...
Gel-Free Tools for Quick and Simple Screening of Anti-Topoisomerase 1 Compounds
(MDPI, 2023-04-27)
With the increasing need for effective compounds against cancer or pathogen-borne diseases, the development of new tools to investigate the enzymatic activity of biomarkers is necessary. Among these biomarkers are DNA ...
Phosphorus substituted hydroxylamine and hydroxamic acid derivatives: synthesis and reactivity
(Arkat USA Inc, 2011)
[EN] This review summarizes several reports concerning the synthesis and synthetic applications of hydroxylamines derived from phosphines, phosphine oxides and phosphonates, and phosphorus substituted hydroxamic acid ...
Novel topoisomerase I inhibitors. Syntheses and biological evaluation of phosphorus substituted quinoline derivates with antiproliferative activity
(Elsevier, 2018-02-22)
This work describes the synthesis of 1,2,3,4-tetrahydroquinolinylphosphine oxides, phosphanes and phosphine sulfides as well as that of quinolinylphosphine oxides and phosphine sulfides, which were synthesized in good to ...
Antileishmanial Effect of 1,5- and 1,8-Substituted Fused Naphthyridines
(MDPI, 2023-12-22)
In the absence of a vaccine, there is a need to find new drugs for the treatment of neglected tropical diseases, such as leishmaniasis, that can overcome the many drawbacks of those currently used. These disadvantages ...
Synthesis of novel antiproliferative hybrid bis-(3-indolyl)methane phosphonate derivatives
(Elsevier, 2018-09-15)
An efficient synthetic methodology for the preparation of phosphorus substituted bis-(3-indolyl)methane through a double nucleophilic addition of indole derivatives to an in situ generated α-iminophosphonate is reported. ...
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 ...
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 ...