264611-42-9Relevant articles and documents
Customizable and Regioselective One-Pot N?H Functionalization of DNA Nucleobases to Create a Library of Nucleobase Derivatives for Biomedical Applications
Borges, Jo?o,Machado, Carmen M.,Mano, Jo?o F.,Rocha, Djenisa H. A.,Silva, Artur M. S.,Silva, Vera L. M.,Sousa, Cristiana F. V.,Sousa, Vera
, p. 4423 - 4433 (2021)
DNA is one of the most exciting biomolecules in nature for developing supramolecular biofunctional nanoarchitectures owing to the highly specific and selective interactions between complementary Watson-Crick base pairing. Herein, simple and one-pot synthetic procedures have been implemented for producing a library of DNA nucleobase derivatives endowed with reactive functional groups for bioconjugation and cross-linking strategies with other (bio)molecules. Purine and pyrimidine molecules have been regioselectively N?H functionalized either via N-alkylation, N-allylation, N-propargylation or Michael-type reactions and structurally characterized. The influence of the reaction conditions was assessed and discussed. The in vitro biocompatibility of the native and nucleobase derivatives was evaluated by culturing them with human fibroblasts, revealing their cytocompatibility. The library of nucleobase derivatives holds great promise for being coupled to different biomolecules, including biopolymeric materials, lipids, and peptides, thus potentially leading to modular supramolecular nanobiomaterials for biomedicine.
Nucleoside base derivative and preparation method and application thereof
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Paragraph 0059-0063, (2021/01/29)
The invention belongs to the field of medicines, and relates to a nucleoside base derivative with P300 acetylase selective inhibition activity and application thereof. The nucleoside base derivative is a compound with a structure shown as a formula I, a compound with a structure shown as a formula II, or a tautomer, an enantiomer, a diastereoisomer, a meso-racemate, a raceme or a mixture thereof,or a prodrug thereof, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Researches show that the compounds shown in the formula I and the formula II have good inhibitory activity on P300 acetylase, show good selectivity on CBP, have a small cytotoxic effect, and can be used as probe molecules and lead compounds for P300 acetylase action mechanism research and P300 related diseasedrug research and development.
Synthesis and in vitro activity of N-sulfonylamidine-derived Pyrimidine Analogues
Krstulovi?, Luka,Safti?, Dijana,Ismaili, Hamit,Baji?, Miroslav,Glava?-Obrovac, Ljubica,?ini?, Biserka
, p. 625 - 636 (2018/05/07)
Two novel series of N-sulfonylamidino pyrimidine derivatives were synthesized via Cu-catalyzed three-component reaction of propargylated nucleobases with different benzenesulfonyl azides and amines. In this way 4-acetamido, 4 -methyl and 4-carboxybenzenesulfonyl amidine products 15-26 in the uracil series and 4-acetamidobenzenesulfonyl amidine derivatives 27-29 in the cytosine series were prepared in 34-69 % yields. Attempts to prepare N-sulfonylamidino cytosine derivatives in reaction with 4-methylbenzenesulfonyl azide were unsuccessful. The cytosine derivatives 32 and 33 were prepared from the N-sulfonylamidino uracil derivatives via the C4 triazole intermediates. The prepared N-sulfonylamidino pyrimidine derivatives 1-28 were tested for the antiproliferative activity on a panel of seven tumor cell lines of different histological origin (HeLa, Caco-2, NCI-H358, Raji, HuT78, K562, Jurkat) and on normal MDCK I cells. Most of the synthesized compounds showed antiproliferative activity on the tested cell lines.
