Ring-Substituted y1,2-Bis(4-hydroxyphenyl)ethylenediamine>dichloroplatinum(II) Complexes: Compounds with a Selective Effect on the Hormone-Dependent Mammary Carcinoma

Article abstract of DOI:10.1021/jm00396a012

<1,2-Bis(4-hydroxyphenyl)ethylenediamine>dichloroplatinum(II) complexes with one substituent in the 2-position (CH3, CF3, F, Br, I: meso- and dl-1-PtCl2, meso-(3-5)-PtCl2, meso-(7 and 8)-PtCl2) or two substituents in the 2,6-position (CH3, Cl: meso-2-PtCl2, meso- and dl-6-PtCl2) in both benzene rings were synthesized and tested for estrogenic and toxic activities.Two complexes (meso-6-PtCl2 and meso-7-PtCl2) possess both effects.In comparative tests on estrogen receptor positive and negative mammary tumors in cell culture (MCF 7, ER⁺ and MDA-MB 231, ER^-) and in animals (MXT, ER⁺ and MXT, ER^-, mouse), meso-6-PtCl2 shows a selective effect on the estrogen receptor positive mammary carcinoma.A further increase of efficacy was achieved with the water-soluble (sulfato)platinum(II) derivative (meso-6-PtSO4).On the DMBA-induced hormone dependent mammary carcinoma of the SD rat, meso-6-PtSO4 is significantly more active than its ligand (meso-6) and cisplatin.