Semi-synthesis and Biological Activity of new D-ring modified camptothecins

摘要

For the past three decades the 20(S)-Camptothecin alkaloid has engaged the special attention of medicinal chemists and pharmacologists due to its promising anti-cancer activity against the most aggressive histotypes. However, the relative water insolubility of CPT and its considerable toxicity in clinical trials, have led to the development of a number of A-, B-and E-ring camptothecin derivatives.1 So far, reports on the synthesis of C and D rings modified analogs are lacking, besides among these compounds, only the 14-azacamptothecin exhibited a reasonable potency as a topoisomerase I poison.