Synthesis and Biological Properties of 5-(1H-1,2,3-Triazol-4-yl)isoxazolidines: A New Class of C-Nucleosides

Molecules

Salvatore V. Giofrè¹  Santa Cirmi¹  Roberto Romeo¹  Caterina Carnovale¹  Michele Navarra¹  Maria A. Chiacchio²  Raffaella Mancuso³  Adriana Garozzo⁴ 

[1] Dipartimento Scienze del Farmaco e Prodotti per la Salute, Università di Messina,Via S.S. Annunziata, Messina 98168, Italy;Dipartimento Scienze del Farmaco, Università di Catania, Viale A. Doria 6, Catania 95125, Italy;Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria, Via P. Bucci, 12/C, Arcavacata di Rende (CS) 87036, Italy;Dipartimento di Scienze Bio-mediche, Università di Catania, Via Androne 81, Catania 95124, Italy;

关键词: vinyl triazoles;    C-Nucleosides;    1,3-dipolar cycloaddition;    antiproliferative activity;    microwave;   

DOI  :  10.3390/molecules20045260

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown