title: Ring-substituted [1,2-bis(4-hydroxyphenyl)ethylenediamine]dichloroplatinum (II) complexes: compounds with a selective effect on the hormone-dependent mammary carcinoma.
abstract: [1,2-Bis(4-hydroxyphenyl)ethylenediamine]dichloroplatinum (II) complexes with one substituent in the 2-position (CH3, CF3, F, Cl, Br, I: meso- and d,l-1-PtCl2, meso-(3-5)-PtCl2, meso-(7 and 8)-PtCl2) or two substituents in the 2,6-positions (CH3, Cl: meso-2-PtCl2, meso- and d,l-6-PtCl2) in both benzene rings were synthesized and tested for estrogenic and cytotoxic 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.
authors.affiliation: Institut für Pharmazie, Universität Regensburg, Federal Republic of Germany.
authors.forename: J
authors.initials: J
authors.lastname: Karl
authors.forename: R
authors.initials: R
authors.lastname: Gust
authors.forename: T
authors.initials: T
authors.lastname: Spruss
authors.forename: M R
authors.initials: MR
authors.lastname: Schneider
authors.forename: H
authors.initials: H
authors.lastname: Schönenberger
authors.forename: J
authors.initials: J
authors.lastname: Engel
authors.forename: K H
authors.initials: KH
authors.lastname: Wrobel
authors.forename: F
authors.initials: F
authors.lastname: Lux
authors.forename: S T
authors.initials: ST
authors.lastname: Haeberlin
mesh_terms: D000818:Animals; D001943:Breast Neoplasms; D002460:Cell Line; D002945:Cisplatin / Q000627:therapeutic use; D005260:Female; D006801:Humans; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy*; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D009944:Organoplatinum Compounds; D002945:Cisplatin