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Platinum complexes with binding affinity for the estrogen receptor

Knebel, N. ; Angerer, E. von


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.

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