Advances in the Chemistry of Tumor-Inhibitory Natural Products

Abstract

The discovery of the antileukemic activity of nitrogen mustard in the 1940’s is considered by many to have been the start of modern cancer chemotherapy². An enormous amount of work has followed on the synthesis and evaluation of biological alkylating agents^25-28. Although the preparation of modifications of presently-known alkylating agents continues, some pessimism is evident among workers in the field. The extensive synthetic efforts to date have led only to minimal improvements over the prototype drugs. Evidently, the high degree of reactivity of simple alkylating agents leads to indiscriminate reactions with many cell constituents and, consequently, narrow therapeutic indices. There exists a need for new prototypes for the synthetic organic chemist to use in the design of selective alkylating agents.