GUST, R and SCHONENBERGER, H (1993) SYNTHESIS AND EVALUATION OF THE ANTI-MAMMARY TUMOR-ACTIVITY AND OF THE ESTROGENIC SIDE-EFFECTS OF [1,2-BIS(2,6-DIHALO-3-HYDROXYPHENYL)ETHYLENEDIAMINE]PLATINUM(II) COMPLEXES. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 28 (2). pp. 103-115. ISSN 0223-5234,
Full text not available from this repository.Abstract
The synthesis and structural characterization of mammary tumor-inhibiting, diastereomeric [1,2-bis(2,6-dihalo-3-hydroxyphenyl) ethylenediamine]platinum(II) complexes with 2,6-Cl2, 2-F, 6-Cl, 2-Cl, 6-F and 2,6-F2 substituents (1-PtSO4 to 4-PtSO4) are described. The related 1,2-diphenylethylenediamines (1-4) are synthesized by stereoselective meso-meso and D,L-D,L diaza-Cope-rearrangement reactions and coordinated to platinum(II) with K2PtI4 (1-PtI2 to 4-PtI2). The subsequent reaction with Ag2SO4 leads to the respective sulfatoplatinum(II) complexes. They were tested for their anti-tumor activities on die hormone-sensitive and- insensitive MXT mammary carcinoma implanted in mice (MXT-MC, ER+ and MXT-MC, ER-). Complexes with F atoms in the neighborhood of the 3-hydroxy group showed strong inhibitory effects on the MXT-MC, ER+. The best effects were found for the diastereomeric 2,6-F2-substituted complexes, meso-4-PtSO4 and D,L-4-PtSO4. These complexes are strongly active both on the MXT-MC, ER+ and the MXT-MC, ER- and cause no estrogenic side effects.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | INHIBITING <1,2-BIS(FLUOROPHENYL)ETHYLENEDIAMINE>PLATINUM(II) COMPLEXES; ACETOXY-SUBSTITUTED 1,1,2-TRIPHENYLBUT-1-ENES; BIOLOGICAL EVALUATION; RING; ANTITUMOR; CARCINOMA; LEUKEMIA; LIGANDS; SULFATE; CANCER; 1,2-DIPHENYLETHYLENEDIAMINES; PLATINUM(II) COMPLEXES; ANTITUMOR ACTIVITY; ESTROGENIC SIDE EFFECT |
| Depositing User: | Dr. Gernot Deinzer |
| Last Modified: | 19 Oct 2022 08:43 |
| URI: | https://pred.uni-regensburg.de/id/eprint/54181 |
Actions (login required)
 |
View Item |
