New analogues of the antitumor alkaloid girolline: The 4-deazathiogirolline series

被引：5

作者：

Nay, B ^{[1
]}

Schiavi, B ^{[1
]}

Ahond, A ^{[1
]}

Poupat, C ^{[1
]}

Potier, P ^{[1
]}

机构：

[1] CNRS, Inst Chim Subst Nat, F-91198 Gif Sur Yvette, France

来源：

SYNTHESIS-STUTTGART | 2005年 / 01期

关键词：

girolline; aminothiazole; chiral pool; antitumor; structure-activity relationships;

D O I：

10.1055/s-2004-834907

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Aminothiazole analogues of the antitumor alkaloid girolline have been asymmetrically synthesised using the chiral pool. The key-steps involved the Hantzsch reaction to build the thiazole heterocycle and the functionalisation of the side chain using the triphenylphosphane chemistry (i.e. azidation-chlorination of a diol). Biological activity of analogues has been evaluated (cytotoxicity on KB tumor cells and anti-HIV activity).

引用

页码：97 / 101

页数：5

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