1. Synthesis and biological properties of 5-(1H-1,2,3-triazol-4-yl)isoxazolidines: a new class of C-nucleosides.
- Author
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Giofrè SV, Romeo R, Carnovale C, Mancuso R, Cirmi S, Navarra M, Garozzo A, and Chiacchio MA
- Subjects
- Antineoplastic Agents chemistry, Cell Proliferation drug effects, Drug Screening Assays, Antitumor, HT29 Cells, Hep G2 Cells, Humans, Isoxazoles chemistry, Molecular Mimicry, Molecular Structure, Nucleosides chemical synthesis, Nucleosides chemistry, Nucleosides pharmacology, Pyrimidines chemistry, Structure-Activity Relationship, Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Isoxazoles chemical synthesis, Isoxazoles pharmacology
- Abstract
A novel series of C-nucleosides, featuring the presence of a 1,2,3-triazole ring linked to an isoxazolidine system, has been designed as mimetics of the pyrimidine nucleobases. An antiproliferative effect was observed for compounds 17a and 17b: the growth inhibitory effect reaches the 50% in HepG2 and HT-29 cells and increases up to 56% in the SH-SY5Y cell line after 72 h of incubation at a 100 µM concentration.
- Published
- 2015
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