Platinum complexes with binding affinity for the estrogen receptor

J Med Chem. 1988 Sep;31(9):1675-9. doi: 10.1021/jm00117a002.

Abstract

A number of (1,2-diaminoethane)dichloroplatinum(II) complexes, linked to dihydroxy-2-phenylindole by spacer groups of varying lengths, were synthesized and studied for their binding affinities for the calf uterine estrogen receptor. Best binding conditions were provided by the n-hexyl and the p-xylene group as spacer with RBA values of 6.5 (16c) and 4.4 (17c), respectively (17 beta-estradiol: RBA = 100). These values are only slightly lower than those of the corresponding diaminoethane ligands.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents
  • Binding, Competitive
  • Cattle
  • Chemical Phenomena
  • Chemistry
  • Cytosol / metabolism
  • Estradiol / metabolism
  • Female
  • Organoplatinum Compounds / chemical synthesis
  • Organoplatinum Compounds / metabolism*
  • Receptors, Estrogen / metabolism*
  • Uterus / metabolism

Substances

  • Antineoplastic Agents
  • Organoplatinum Compounds
  • Receptors, Estrogen
  • platinum ethylenediamine dichloride
  • Estradiol