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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 ...
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 ...
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. ...
Phosphinotripeptidic Inhibitors of Leucylaminopeptidases
(MDPI, 2021-05-11)
Phosphinate pseudopeptide are analogs of peptides containing phosphinate moiety in a place of the amide bond. Due to this, the organophosphorus fragment resembles the tetrahedral transition state of the amide bond hydrolysis. ...
Sc(OTf)(3)-Mediated [4+2] Annulations of N-Carbonyl Aryldiazenes with Cyclopentadiene to Construct Cinnoline Derivatives: Azo-Povarov Reaction
(American Chemical Society, 2022)
We disclose the first accomplishment of the azo-Povarov reaction involving Sc(OTf)3-catalyzed [4 + 2] annulations of N-carbonyl aryldiazenes with cyclopentadiene in chloroform, in which N-carbonyl aryldiazenes act as ...
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 ...