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

Bis-naphthalimidopropyl putrescine (BNIPPut), spermidine (BNIPSpd), spermin e (BNIPSpm) and oxa-putrescine (BNIPOPut) were synthesised and their growth -inhibitory properties characterised. All these compounds except for BNIPOP ut, showed high in vitro cytotoxic activity (with mean GI(50) values betwee n 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 li nker chain of BNIPSpd and BNIPSpm significantly improved their aqueous diss olution properties with a marginal decrease in their cytotoxic activity. (C ) 2000 Elsevier Science Ltd. All rights reserved.