Synthesis and Antitumor Activity of 7-Substituted 20(RS)-Camptothecin Analogues.

Novel water-soluble camptothecin analogues with excellent antitumor activity have been designed and synthesized by total synthesis. The analogues were evaluated for cytotoxic activity against five tumor cell lines. The most potent analogue 6c exhibited significant antitumor activity at wider range of doses as compared with camptothecin (T/C 243 % at 70mg/kg; T/C > 150% at 8.75–140mg/kg).