Dichloro[1,2-bis(4-hydroxyphenyl)ethylenediamine]platinum(II) complexes: an approach to develop compounds with a specific effect on the hormone-dependent mammary carcinoma.
Stereoisomeric dichloro [1,2-bis(4-hydroxyphenyl)ethylenediamine]platinum(II) complexes (meso-3a, (+/-)-3b, (+)-3c, (-)-3d) and their N,N'-dibutyl derivatives (meso-4a, (+/-)-4b, (+)-4c, (-)-4d) were synthesized and tested on antitumor activity. The most active compound, 3d, shows a modest inhibition of the [3H]estradiol receptor interaction and causes a marked effect on the growth of the hormone-dependent human MCF 7 breast cancer cell line. It is also active on the hormone-independent human MDA-MB 231 breast cancer cell line, on the ADJ/PC6 plasmacytoma of the Balb/C mouse, and on the L 5222 leukemia of the BD IX rat. Apparently the inhibition of the MCF 7 cell line is not mediated by the estrogen receptor system. Histopathological studies on 3d revealed very low toxicity.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D001943:Breast Neoplasms / Q000473:pathology*; D002460:Cell Line; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004958:Estradiol / Q000378:metabolism; D005260:Female; D006801:Humans; D007202:Indicators and Reagents; D007942:Leukemia, Experimental / Q000473:pathology; D051379:Mice; D008807:Mice, Inbred BALB C; D008968:Molecular Conformation; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000633:toxicity; D010954:Plasmacytoma / Q000473:pathology; D051381:Rats; D011919:Rats, Inbred Strains; D011959:Receptors, Estradiol / Q000032:analysis; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D009944:Organoplatinum Compounds; D011959:Receptors, Estradiol; D004958:Estradiol; C042922:dichloro(1,2-bis(4-hydroxyphenyl)ethylenediamine)platinum II