Synthesis and Anti-tumour Activity in Vitro of Camptothecin-Bile ACID analogues

摘要

Aim: Synthesis a series of camptothecin-bile acids derivatives. Method: Bile acid were combined with camptothecin by ester reaction at the presence of double agent. Result: Some of these derivatives showed cytotoxic activity comparable to that of camptothecin in human liver and colon cancer cells. The cytotoxic activities of these derivatives against bile acid-negative Hela cells were much lower than that against the bile acid- positive liver and colon cancer cells. The lactone stability of these tested derivatives in rat blood serum was generally improved.