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

Add time:08/19/2019    Source:sciencedirect.com

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 the 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.

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