Synthesis and cytotoxic activities of estrone and estradiol cis-dichloroplatinum(II) complexes
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
23142322
DOI
10.1016/j.bmc.2012.10.013
PII: S0968-0896(12)00823-1
Knihovny.cz E-resources
- MeSH
- Estradiol analogs & derivatives chemical synthesis chemistry pharmacology MeSH
- Estrone analogs & derivatives chemical synthesis chemistry pharmacology MeSH
- Coordination Complexes chemical synthesis chemistry pharmacology MeSH
- Humans MeSH
- Ligands MeSH
- MCF-7 Cells MeSH
- Cell Line, Tumor MeSH
- Organoplatinum Compounds chemical synthesis chemistry pharmacology MeSH
- Antineoplastic Agents chemical synthesis chemistry pharmacology MeSH
- Drug Screening Assays, Antitumor MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Estradiol MeSH
- Estrone MeSH
- Coordination Complexes MeSH
- Ligands MeSH
- Organoplatinum Compounds MeSH
- Antineoplastic Agents MeSH
Sixteen platinum(II) complexes of estrone and estradiol were synthesized in this work to evaluate their cytotoxic activity against several cancer cell lines including estrogen dependent and independent ones. The synthesis of all the complexes was done in three steps. The reaction of steroids with dibromoalkanes was followed by a reaction of the bromoalkyl steroids with 2-(aminomethyl)pyridine or 2-(2-aminoethyl)pyridine. The last step was a reaction of steroidal diamino ligands with potassium tetrachloroplatinate to obtain the desired platinum(II) complexes. Cytotoxicity assays showed that most of the complexes prepared are active against the cancer cell lines used-CEM, U-2 OS, MCF7, MCF7 AL, MDA-MB-468, BT-474, BT-549, and BJ fibroblasts. The six-membered platinum complexes are more active than five-membered ones.
References provided by Crossref.org
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