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嘌呤碱氮芥衍生物的合成及生物学评价

Synthesis and biological evaluation of nitrogen mustard derivatives of purine bases.

作者信息

Boëns Benjamin, Azouz Mounir, Ouk Tan-Sothea, Zerrouki Rachida

机构信息

Laboratoire de Chimie des Substances Naturelles, Limoges, France.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2013;32(2):69-80. doi: 10.1080/15257770.2013.763977.

DOI:10.1080/15257770.2013.763977
PMID:23448142
Abstract

This paper deals with the synthesis of nitrogen mustard analogs, derivatives of purine bases. Alkylation in position N-9 and diethanolamine fixation on position 6 were managed by microwave irradiations. Chlorination of these dihydroxylated intermediates led to a cyclization, giving tricyclic purine base analogs bearing a chloroethyl chain. Finally, MTT assays on obtained compounds do not show cytotoxicity on four different cancer cell lines.

摘要

本文涉及氮芥类似物(嘌呤碱衍生物)的合成。通过微波辐射实现了N - 9位的烷基化和6位的二乙醇胺固定。这些二羟基化中间体的氯化导致环化,生成带有氯乙基链的三环嘌呤碱类似物。最后,对所得化合物进行的MTT测定表明,其对四种不同的癌细胞系均无细胞毒性。

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