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作为抗肿瘤药物的“最小化”DNA嵌入剂:安吖啶的2-苯乙烯基喹啉类似物

'Minimal' DNA-intercalating agents as anti-tumour drugs: 2-styrylquinoline analogues of amsacrine.

作者信息

Denny W A, Atwell G J, Baguley B C

机构信息

Cancer Research Laboratory, University of Auckland School of Medicine, New Zealand.

出版信息

Anticancer Drug Des. 1987 Dec;2(3):263-70.

PMID:3449090
Abstract

A series of analogues of amsacrine have been prepared by replacing the acridine with a variety of other chromophores, in a search for 'minimal' DNA-intercalating anti-tumour agents which might show superior distributive properties as a consequence of lower levels of binding to cellular macromolecules. 2-Styrylquinoline derivatives did show in vivo anti-leukaemic activity, but none of the compounds was superior to amsacrine itself.

摘要

通过用多种其他发色团取代吖啶,制备了一系列安吖啶类似物,以寻找 “最小化” 的DNA嵌入抗肿瘤剂,由于与细胞大分子的结合水平较低,这些药剂可能具有更好的分布特性。2-苯乙烯基喹啉衍生物确实显示出体内抗白血病活性,但没有一种化合物优于安吖啶本身。

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