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Now showing items 11-20 of 32
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 ...
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 ...
A Multicomponent Protocol for the Synthesis of Highly Functionalized γ-Lactam Derivatives and Their Applications as Antiproliferative Agents
(MDPI, 2021-08-09)
An efficient synthetic methodology for the preparation of 3-amino 1,5-dihydro-2H-pyrrol-2-ones through a multicomponent reaction of amines, aldehydes, and pyruvate derivatives is reported. In addition, the densely substituted ...
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 ...
syn-Selective Michael reaction of α-branched aryl acetaldehydes with nitroolefins promoted by squaric amino acid derived bifunctional Brønsted bases
(Wiley, 2021-07-07)
[EN] Here we describe a direct access to 2,2,3-trisubstituted syn γ-nitroaldehydes by addition of α-branched aryl acetaldehydes to
nitroolefins promoted by a cinchona based squaric acid-derived
amino acid peptide. Different ...
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 ...
Asymmetric Synthesis of Tetrasubstituted α-Aminophosphonic Acid Derivatives
(MDPI, 2021-05-27)
Due to their structural similarity with natural α-amino acids, α-aminophosphonic acid derivatives are known biologically active molecules. In view of the relevance of tetrasubstituted carbons in nature and medicine and the ...
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. ...
Late-Stage C-H Acylation of Tyrosine-Containing Oligopeptides with Alcohols
(American Chemical Society, 2021-09-17)
The selective tagging of amino acids within a peptide framework while using atom-economical C-H counterparts poses an unmet challenge within peptide chemistry. Herein, we report a novel Pd-catalyzed late-stage C-H acylation ...