Strategy and tactics of chemotherapeutic drug development.

Strategic approaches to generating chemotherapeutically active lead compounds are either empirical as in traditional synthetic programs or in the search for antibiotics; they are semiempirical as concerns the design of antimetabolites and more rational for the design of DNA-complexing drugs. The tactics of exploitation of active lead compounds in chemotherapeutic drug development involve molecular modification. This aims at either substances with greater activity and/or substances with improved pharmacokinetic parameters. From quantitative structure-activity relationships one might extrapolate to members of a chemical series with improved pharmacokinetic properties. Scientific advances render chemotherapy research more predictive and, hence, less empirical.