Camptothecin (1) is a plant anti-tumor agent of novel structure which exhibited promising anti-tumor activity in animal models. In clinical practice 1 was utilized as the water soluble sodium salt 7 in the belief that it was of equivalent activity to 1. Recent data indicate that 7 is much less active. Compound 7 was not effective in man against leukemia or GI carcinomas. We propose the synthesis of analogs of 1 which would contain water solubilizing groups or groups which can form water soluble derivatives and in all cases retaining the intact lactone ring E. To achieve this aim, we propose to synthesize a versatile tricyclic intermediate containing rings C, D, E or 1 which can be converted into 1, and a variety of pentacyclic and tetracyclic analogs. (2) 1 and its desoxy analog are receiving intense study as biochemical and metabolic tools. Synthesis of labeled 1 or analogs will be of greater help to workers in this area. (3) We wish to study the reaction of labeled 1 with appropriate nucleophiles in order to achieve a greater understanding of why RNA and DNA are reversibly inhibited by 1 and analogs.