Chemistry of Camptothecin and its Related Alkaloids

Overview of the recent progress on the chemical studies of antitumor alkaloid, camptothecin (CPT), and its close relatives is described. This article covers 1) isolation and synthesis of possible biosynthetic intermediates of CPT starting from an indole alkaloid, strictosamide, 2) recent total synthesis of racemic and chiral CPT, and 3) a mechanism of anticancer action of CPT using the Topo I-DNA-CPT ternary complex model, which was proposed on the basis of chemical and biochemical information combined with the X-ray crystal structure of the complex of Topo I and DNA, as well as recent medicinal chemistry studies on the development of potent anticancer chemotherapeutics having camptothecinoid structures.