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.
Nucleoside and base hydroxamic acid derived compound and preparation method and applications thereof
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Paragraph 0107; 0108; 0109; 0110, (2017/08/29)
The invention discloses a nucleoside and base hydroxamic acid compound with DNA transmethylase and/or histone deacetylase inhibition activity, and a preparation method and applications thereof. The structural formula of the nucleoside and base hydroxamic acid compound is shown as the formula I, wherein R is nucleoside and base, nucleoside and base with substituent group or nucleoside and base analogue in DNA and/or RNA; Linker is a connecting chain connecting R with hydroxamic acid function group, the connecting chain comprises but is not limited within alkyl chain, alkyl chain with heteroatom, alkyl chain with aromatic ring, and alkyl chain with heterocycle. In-vitro cell proliferation assay show that the compound shown in the formula I can well inhibit the proliferation of leukemia cell K562 and histocyte lymphoma cell U937. Transmethylase and histone deacetylase inhibition assay shows that the compound shown in the formula I is a compound having inhibition activity on the DNA transmethylase and/or histone deacetylase. The formula I is as shown in the specification.
