Prodrugs of Ara-CMP and Ara-AMP with a S-acyl-2-thioethyl (SATE) biolabile phosphate protecting group:: Synthesis and biological evaluation

被引：9

作者：

Bazzanini, R

Manfredini, S

Durini, E

Gröschel, B

Cinatl, J

Balzarini, J

De Clercq, E

Imbach, JL

Périgaud, C

Gosselin, G

机构：

[1] CNR, ICoCEA, I-40129 Bologna, Italy

[2] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy

[3] Univ Frankfurt Klinikum, Inst Med Virol, D-60596 Frankfurt, Germany

[4] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

[5] Univ Montpellier 2, Chim Bioorgan Lab, UMR CNRS USTL 5625, F-34095 Montpellier 5, France

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 1999年 / 18卷 / 4-5期

关键词：

D O I：

10.1080/15257779908041616

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：

The bis(S-pivaloyl-2-thioethyl) phosphotriesters of Ara-C and Ara-A were synthesized as potential bioreversible mononucleotide prodrugs. Some N- and O-acylated derivatives were also prepared with the aim to modify the lipophilicity of the title pronucleotides. Compounds were tested far their antitumor/antiviral activity against a variety of tumor cells and viruses.

引用

页码：971 / 972

页数：2