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  • Title: Aqua[1,1-bis(4-hydroxyphenyl)-1,2-diamino-2-phenylethane]- sulfatoplatinum(II), a new compound for the treatment of the mammary carcinoma.
    Author: Gust R.
    Journal: Arch Pharm (Weinheim); 1994 Jan; 327(1):49-54. PubMed ID: 8117188.
    Abstract:
    The highly estrogen receptor(ER)-affinic compound 1,1-bis(4-hydroxyphenyl)-2-phenylethane (BHPE) was used as carrier ligand for a new cisplatin derivative, aqua[1,1-bis(4-hydroxyphenyl)-1,2-diamino-2-phenylethane]sulfatoplati num (II) (3-PtSO4) for the therapy of the ER-positive (i.e. hormone sensitive) breast cancer. The diamine ligand 1,1-bis(4-hydroxyphenyl)-1,2-diamino-2-phenylethane (3) was synthesized by transformation of the O-methyl ether derivative of BHPE into the 1,2-bisazido compound 3b with IN3/NaN3, reduction of both N3 residues into NH2 groups [3a] and subsequent ether cleavage with BBr3. From the diamine ligand 3 and K2PtI4 a five-membered chelate 3-PtI2 was obtained which was transformed into 3-PtSO4 with Ag2SO4. In comparison to BHPE the ER-affinity of 3-PtSO4 is markedly reduced. 3-PtSO4 possesses, however, weak cytotoxic activity (P388) and antiestrogenic, but no estrogenic properties. 3-PtSO4 is comparable with BHPE in terms of its activity on the hormone sensitive MXT-M 3.2 breast cancer of the mouse.
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