Exploring the Scope of [Pt2(4-FC6H4)4(渭-SEt2)2] as a Precursor for New Organometallic Platinum(II) and Platinum(IV) Antitumor Agents

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• 作者：Anna Escol脿 ; Margarita Crespo ; Josefina Quirante ; Rold谩n Cort茅s ; Anusha Jayaraman ; Josefa Bad铆a ; Laura Baldom脿 ; Teresa Calvet ; Merc猫 Font-Bard铆a ; Marta Cascante
• 刊名：Organometallics
• 出版年：2014
• 出版时间：April 14, 2014
• 年：2014
• 卷：33
• 期：7
• 页码：1740-1750
• 全文大小：495K
• 年卷期：v.33,no.7(April 14, 2014)
• ISSN：1520-6041

文摘

The new compound [Pt₂(4-FC₆H₄)₄(渭-SEt₂)₂] (A) was prepared and fully characterized. The reactions of compound A with ligands ArCH鈺怤CH₂CH₂NMe₂ (Ar = 2-BrC₆H₄, 1a; 2,6-Cl₂C₆H₃, 1b; 4-ClC₆H₄, 1c; 2-Cl,6-FC₆H₃, 1d) were studied under different conditions and produced platinum(II) compounds [Pt(4-FC₆H₄)₂(ArCH鈺怤CH₂CH₂NMe₂)] (2b鈥?b>2d), containing a bidentate [N,N鈥瞉 ligand, as well as cyclometalated platinum(IV) or platinum(II) compounds such as [PtBr(4-FC₆H₄)₂(C₆H₄CH鈺怤CH₂CH₂NMe₂)] (4a) or [PtCl{(3-FC₆H₃)(2-XC₆H₃)CH鈺怤CH₂CH₂NMe₂}] (5b: X = Cl; 5d: X = F), containing a tridentate [C,N,N鈥瞉 ligand and either a five (4a) or a seven (5b, 5d) membered metallacycle. These compounds exhibit a great antiproliferative activity against non-small lung cancer cells (A549), and the best result was obtained for compound 2c (IC₅₀ = 0.3 卤 0.1 渭M). While compounds 5 alter the mobility of plasmid DNA in a similar way to cisplatin, compound 4 was less efficient in removing the supercoils from DNA. In spite of the very low IC₅₀ value obtained for compound 2c, this compound does not interact with DNA, and it is neither an intercalator nor a topoisomerase I inhibitor.