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Hydrogen sulphide-triggered theranostic prodrugs based on the dynamic chemistry of tetrazines
(Royal Society of Chemistry, 2022)
[EN] Dynamic nucleophilic aromatic substitution of tetrazines (S(N)Tz) has been employed to build theranostic prodrugs that are activated by hydrogen sulfide. H2S is typically found in high concentrations in some kinds of ...
Fused 1,5-Naphthyridines: Synthetic Tools and Applications
(MDPI, 2020-07-31)
Heterocyclic nitrogen compounds, including fused 1,5-naphthyridines, have versatile applications in the fields of synthetic organic chemistry and play an important role in the field of medicinal chemistry, as many of them ...
Synthesis of Heterocyclic Fused [1,5]naphthyridines by Intramolecular HDA Reactions
(MDPI, 2019-09-06)
Povarov reaction [1] can be considered as an example of HDA reactions and represents an
excellent method for the preparation of nitrogen-containing heterocyclic compounds [2]. When
aldimines, derived from aromatic amines ...
Synthetic Strategies, Reactivity and Applications of 1,5-Naphthyridines
(MDPI, 2020-07-16)
This review covers the synthesis and reactivity of 1,5-naphthyridine derivatives published in the last 18 years. These heterocycles present a significant importance in the field of medicinal chemistry because many of them ...
A Dual-Sensor-Based Screening System for In Vitro Selection of TDP1 Inhibitors
(MDPI, 2021-07-15)
DNA sensors can be used as robust tools for high-throughput drug screening of small molecules with the potential to inhibit specific enzymes. As enzymes work in complex biological pathways, it is important to screen for ...
Synthesis of hybrid phosphorated indenoquinolines and biological evaluation as topoisomerase I inhibitors and antiproliferative agents
(Elsevier, 2022-02-01)
[EN]This work describes the first synthesis of diethyl 6,6a,7,11b-tetrahydro-5H-indeno[2,1-c]quinolinylphosphonates 5, diethyl 7H-indeno[2,1-c]quinolinylphosphonates 6 and diethyl 7-oxo-7H-indeno[2,1-c]quinolinylphosphonates ...
Hybrid Quinolinyl Phosphonates as Heterocyclic Carboxylate Isosteres: Synthesis and Biological Evaluation against Topoisomerase 1B (TOP1B)
(MDPI, 2021-08-09)
This work describes, for the first time, the synthesis of dialkyl (2-arylquinolin-8-yl)phosphonate derivatives. The preparation was carried out through a direct and simple process as a multicomponent Povarov reaction of ...
Simple and Fast DNA Based Sensor System for Screening of Small-Molecule Compounds Targeting Eukaryotic Topoisomerase 1
(MDPI, 2021-08-13)
Background: Eukaryotic topoisomerase 1 is a potential target of anti-parasitic and anti-cancer drugs. Parasites require topoisomerase 1 activity for survival and, consequently, compounds that inhibit topoisomerase 1 activity ...
Multicomponent Synthesis of Unsaturated γ-Lactam Derivatives. Applications as Antiproliferative Agents through the Bioisosterism Approach: Carbonyl vs. Phosphoryl Group
(MDPI, 2022-04-22)
We report efficient synthetic methodologies for the preparation of 3-amino and 3-hydroxy 3-pyrrolin-2-ones (unsaturated γ-lactams) through a multicomponent reaction of amines, aldehydes and acetylene or pyruvate derivatives. ...
Naphthyridine Derivatives Induce Programmed Cell Death in Naegleria fowleri
(MDPI, 2021-10-01)
Primary amoebic encephalitis (PAM) caused by the opportunistic pathogen Naegleria fowleri is characterized as a rapid and lethal infection of the brain which ends in the death of the patient in more than 90% of the reported ...