The PtoI) complexes of 1,3-diphenylmooane-1,3-diamines @art IV 2' ) were tested for DNA interaction (W-difference spectroscopy, Tables and), for affinity tothe estrogen receptor (calf uterus cytosol; scarcely any affinity), and for cytostatic activity at estrogen independent h4DA-MB 231 cells (Tables and) and estrogen dependent MCF-7 cells gables 5 and 6). The data are compared with those reported for the analogous 1,2-diphenyl&u~-1,2-diamine-Pt(II) complexes: most probably, the cytostatic activity is not mediated by the estrogen receptor.
1,3-Diphenylpmpan
-l,3diamine, 6. Mitt. I): DNS-Wechselwirkung, Estrogenrezeptor-Affhitiit und cytostatische Wirlung v m 1,3-Diphenylprop~n-l,3di~-Pt(I~-Komplexen Die in der 4. Mitt. 2, besduiebenen 1,3-Diphenyl~-1,3-diamin-Pt(n> Komplexe wurden auf Wechselwirkungen mit DNS (UV-Differempehoskopie, Tab. 1 und 2). auf Minitiit zum Estrogenrezeptor (Kalhterus-Cytosol, fast k i n e Affinitit) und auf cytostatische Alaivitit an der Estrogenunabkgigen MDA-MB 231 Zellinie (Tab. 3 und 4 ) bzw. an Ltrogen-abhangigen MCF-7 Zellen (Tab. 5 und 6) gepriift. Die Ergebnisse werden mit Lit. Angaben uber die analogen 1.2-Diphenyl~-l.2-diamin-Pt(II>Komplexe verglichen: die cyostatische Aktivitiit ist sehr wahrscheinlich nicht Estrogenrezqtor-vermittelt . Schdnenberger and his group -3d) have thoroughly investigated the antitumor activities of 1,2-diphenym-1,2-diamines and theirPt(I1) complexes. The results point towards pronounced stereoselectivity and show that conformational rigidity strongly contributes to the binding of these complexes at the estrogen receptor. As the PtoI) complexes of the CHz-homologous 1,3-diphenyl~-1,3-diamines with a six-membered Pt-containing ring are probably more flexible than the five-membered rings of the 1,2diphenylw-1,2-diamine-Pt(II) complexes, we have synthesized 4, the pertinent ligands as well as their PtflI) complexes 2, and have determined ') Dedicated with warm regards to Prof. Dr. MOhrle, Diisseldorf, on the