Lin P K, Pavlov V A
The Robert Gordon University, School of Applied Sciences, Aberdeen, Scotland, UK.
Bioorg Med Chem Lett. 2000 Jul 17;10(14):1609-12. doi: 10.1016/s0960-894x(00)00293-6.
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 GI50 values between 0.5 and 8.45 microM) 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.
合成了双萘二甲酰亚胺丙基腐胺（BNIPPut）、亚精胺（BNIPSpd）、精胺（BNIPSpm）和氧杂腐胺（BNIPOPut），并对它们的生长抑制特性进行了表征。除BNIPOPut外，所有这些化合物均表现出高体外细胞毒性活性（平均GI50值在0.5至8.45微摩尔之间）以及对源自九种不同人类肿瘤的癌细胞的选择性。BNIPSpd和BNIPSpm连接链中氮原子含量的增加显著改善了它们的水溶出特性，同时其细胞毒性活性略有下降。
