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Synthesis and cytotoxic activities of estrone and estradiol cis-dichloroplatinum(II) complexes
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SYSNO ASEP 0384104 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Synthesis and cytotoxic activities of estrone and estradiol cis-dichloroplatinum(II) complexes Author(s) Kvasnica, Miroslav (UOCHB-X) RID
Rárová, L. (CZ)
Oklešťková, Jana (UEB-Q) RID, ORCID, SAI
Buděšínský, Miloš (UOCHB-X) RID, ORCID
Kohout, Ladislav (UOCHB-X)Number of authors 5 Source Title Bioorganic & Medicinal Chemistry. - : Elsevier - ISSN 0968-0896
Roč. 20, č. 24 (2012), s. 6969-6978Number of pages 10 s. Language eng - English Country GB - United Kingdom Keywords steroids ; estrone ; estradiol ; platinum complex ; cytotoxicity Subject RIV CC - Organic Chemistry R&D Projects 1M06030 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) IAA400550801 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR) Institutional support UOCHB-X - RVO:61388963 ; UEB-Q - RVO:61389030 UT WOS 000311421300008 DOI 10.1016/j.bmc.2012.10.013 Annotation 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. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Year of Publishing 2013
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