Synthesis and cytotoxicity of water soluble quaternary salt derivatives of camptothecin.
In an effort to improve the water solubility of camptothecin, 16 water soluble 10-substituted quaternary ammonium salt derivatives of camptothecin were prepared. Their antitumor activity was evaluated on cancer cells in vitro. All of these salts possess lower cytotoxicities than CPT in comparison. The camptothecin salts 16, 20 showed similar cytotoxic activity to topotecan. Especially the salts 21 showed similar cytotoxic activity to CPT in vitro.
Zu
Yuan-gang
YG
Key Laboratory of Forest Plant Ecology (Northeast Forestry University), Ministry of Education, Harbin 150040, China. zygorl@public.hr.hl.cn
Li
Qing-yong
QY
Fu
Yu-jie
YJ
Wang
Wei
W
D002166:Camptothecin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects*; D006801:Humans; D007624:KB Cells; D015394:Molecular Structure; D012492:Salts / Q000494:pharmacology; D012995:Solubility; D013329:Structure-Activity Relationship; D014867:Water
D012492:Salts; D014867:Water; D002166:Camptothecin