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

被引：27

作者：

Giofre, Salvatore V. ^{[1
]}

Romeo, Roberto ^{[1
]}

Carnovale, Caterina ^{[1
]}

Mancuso, Raffaella ^{[2
]}

Cirmi, Santa ^{[1
]}

Navarra, Michele ^{[1
]}

Garozzo, Adriana ^{[3
]}

Chiacchio, Maria A. ^{[4
]}

机构：

[1] Univ Messina, Dipartimento Sci Farmaco & Prod Salute, I-98168 Messina, Italy

[2] Univ Calabria, Dipartimento Chim & Tecnol Chim, I-87036 Arcavacata Di Rende, CS, Italy

[3] Univ Catania, Dipartimento Sci Biomed, I-95124 Catania, Italy

[4] Univ Catania, Dipartimento Sci Farmaco, I-95125 Catania, Italy

来源：

MOLECULES | 2015年 / 20卷 / 04期

关键词：

vinyl triazoles; C-Nucleosides; 1; 3-dipolar cycloaddition; antiproliferative activity; microwave; PHOSPHONATED CARBOCYCLIC 2'-OXA-3'-AZANUCLEOSIDES; ANALOGS; APOPTOSIS;

D O I：

10.3390/molecules20045260

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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 mu M concentration.

引用

页码：5260 / 5275

页数：16

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