Synthesis and Anti-Tumour Activity of Novel Camptothecin-Bile Acid Analogues

A series of camptothecin-bile acids derivatives of were prepared. 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. Competition assays indicated that bile acids played an important role to carry the derivatives into the bile acid-positive cancer cells. The results suggest that the introduction of bile acids in the 20th position of camptothecin promote the anti-tumour targeting activity of these derivatives to liver cancer cells.