GUST, R (1994) AQUA[1,1-BIS(4-HYDROXYPHENYL)-1,2-DIAMINO-2-PHENYLETHANE]-SULFATOPLATINUM(II), A NEW COMPOUND FOR THE TREATMENT OF THE MAMMARY-CARCINOMA. ARCHIV DER PHARMAZIE, 327 (1). pp. 49-54. ISSN 0365-6233,
Full text not available from this repository.Abstract
The highly estrogen receptor(ER)-affinic compound 1,1-bis(4-hydroxyphenyl)-2-phenylethene (BHPE) was used as carrier ligand for a new cis-platin derivative, aqua[1,1-bis(4-hydroxyphenyl)-1,2-diamino-2-phenylethane]sulfatoplatinum(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 NH, 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,
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | TUMOR INHIBITING ACTIVITY; ACETOXY-SUBSTITUTED 1,1,2-TRIPHENYLBUT-1-ENES; RECEPTOR AFFINITY; ANTI-ESTROGENS; COMPLEXES; |
| Depositing User: | Dr. Gernot Deinzer |
| Last Modified: | 19 Oct 2022 08:41 |
| URI: | https://pred.uni-regensburg.de/id/eprint/53529 |
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