Design and synthesis of multisubstrate analog inhibitors of one-carbon transfer reactions

The design and synthesis of multisubstrate analog enzyme inhibitors offer new opportunities in the creation of potent, highly specific drug molecules. Selected examples of inhibitors of 1-carbon transfer serve to illustrate the potential of this approach. Inhibitors of indole-N-methyltransferase, L-aspartyl transcarbamoylase, and thymidylate synthase are illustrative of many compounds that have demonstrated considerable specificity and potency. Several of these inhibitors and the rationale for their syntheses are described.