Thymidylate synthase inhibitors.

  title={Thymidylate synthase inhibitors.},
  author={Nikolaos Touroutoglou and Richard Pazdur},
  journal={Clinical cancer research : an official journal of the American Association for Cancer Research},
  volume={2 2},
Folate analogues that inhibit thymidylate synthase (TS) selectively were developed based on TS and folate molecular structures and properties. The structure-activity relationship, preclinical and clinical development, and issues of potential importance in the future success of these TS inhibitors are reviewed herein. Properties of these new compounds depend mainly on the use of the reduced folate carrier (RFC) proteins for cellular entry and on intracellular polyglutamation, which augments TS… CONTINUE READING