Structure-activity relationship of ligands of the pyrimidine nucleoside phosphorylases

Academic Article


  • Eighty-seven pyrimidine base and nucleoside analogs were evaluated as inhibitors of uridine phosphorylase (UrdPase) and thymidine phosphorylase (dThdPase). These findings, together with an extensive literature review, have allowed construction of structure-activity relationships for the binding of ligands to UrdPase and dThdPase and provide a basis for the rational design of new inhibitors of these enzymes. Additionally, 2,6-pyridinediol and 6-benzyl-2-thiouracil have been identified as being potent inhibitors of UrdPase and dThdPase respectively. © 1983.
  • Published In

    Digital Object Identifier (doi)

    Author List

  • Niedzwicki JG; El Kouni MH; Shih Hsi Chu; Cha S
  • Start Page

  • 399
  • End Page

  • 415
  • Volume

  • 32
  • Issue

  • 3