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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 Brønsted Acid-Catalyzed Multicomponent Reaction for the Synthesis of Highly Functionalized γ-Lactam Derivatives
(MDPI, 2019-08)
Bronsted acids catalyze a multicomponent reaction of benzaldehyde with amines and diethyl acetylenedicarboxylate to afford highly functionalized gamma-lactam derivatives. The reaction consists of a Mannich reaction of an ...
Design and Evaluation of New Phosphorus Substituted Aziridines as Antiproliferative Agents
(MDPI, 2019-08-09)
Covalent bond formation has become a safe and effective strategy applied not only by nature but also by the pharmaceutical industry to improve disease pharmacology. In the history of modern medicine, covalent drugs have ...
Ugi Reaction on α-Phosphorated Ketimines for the Synthesis of Tetrasubstituted α-Aminophosphonates and Their Applications as Antiproliferative Agents
(MDPI, 2021-03-16)
An Ugi three-component reaction using preformed α-phosphorated N-tosyl ketimines with different isocyanides in the presence of a carboxylic acid affords tetrasubstituted α-aminophosphonates. Due to the high steric hindrance, ...
Synthesis and Antiproliferative Activity of Phosphorus Substituted 4-Cyanooxazolines, 2-Aminocyanooxazolines, 2-Iminocyanooxazolidines and 2-Aminocyanothiazolines by Rearrangement of Cyanoaziridines
(MDPI, 2021-07-14)
Several phosphorus-substituted N-acylated cyanoaziridines 2 and N-carbamoylated cyanoziridines 5 were prepared in good to high yields. N-Acylated cyanoaziridines 2 were used, after ring expansion, in an efficient synthesis ...
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 ...