The synthesis and in vitro cytotoxic studies of novel bis-naphthalimidopropyl polyamine derivatives

被引：33

作者：

Kong, P

Lin, T

Pavlov, VA

机构：

[1] Robert Gordon Univ, Sch Appl Sci, Aberdeen AB25 1HG, Scotland

[2] Univ Sofia St Kliment Ohridski, Fac Biol, Dept Human & Anim Physiol, Sofia 1421, Bulgaria

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(00)00293-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Bis-naphthalimidopropyl putrescine (BNIPPut), spermidine (BNIPSpd), spermine (BNIPSpm) and oxa-putrescine (BNIPOPut) were synthesised and their growth-inhibitory properties characterised. All these compounds except for BNIPOPut, showed high in vitro cytotoxic activity (with mean GI(50) values between 0.5 and 8.45 mu M) and selectivity against cancer cells derived from nine different human tumours. The increased content of nitrogen atoms in the linker chain of BNIPSpd and BNIPSpm significantly improved their aqueous dissolution properties with a marginal decrease in their cytotoxic activity. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1609 / 1612

页数：4

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