The synthesis and in vitro cytotoxic studies of novel bis-naphthalimidopropyl polyamine derivatives.
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.
The Robert Gordon University, School of Applied Sciences, Aberdeen, Scotland, UK. p.kong@rgu.ac.uk
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D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D003603:Cytotoxins / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D007094:Imides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D011073:Polyamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011700:Putrescine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013095:Spermidine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology; D013096:Spermine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D003603:Cytotoxins; D007094:Imides; D011073:Polyamines; D015363:Quinolones; D013096:Spermine; D013095:Spermidine; D011700:Putrescine