Platinum complexes with binding affinity for the estrogen receptor.
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.
Knebel
N
N
Institut für Pharmazie, Universität Regensburg, Federal Republic of Germany.
von Angerer
E
E
D000818:Animals; D000970:Antineoplastic Agents; D001667:Binding, Competitive; D002417:Cattle; D055598:Chemical Phenomena; D002621:Chemistry; D003600:Cytosol / Q000378:metabolism; D004958:Estradiol / Q000378:metabolism; D005260:Female; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000378:metabolism*; D011960:Receptors, Estrogen / Q000378:metabolism*; D014599:Uterus / Q000378:metabolism
D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; D011960:Receptors, Estrogen; C002892:platinum ethylenediamine dichloride; D004958:Estradiol