The influence of ancillary ligands on the antitumoral activity of new cyclometallated Pt(II) complexes derived from an ferrocene-pyrazole hybrid

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• 作者：Eva Guillé ; n^a ; Asensio Gonzá ; lez^b ; Pradipta K. Basu^c ; Amrita Ghosh^c ; Mercè ; Font-Bardia^d ; Teresa Calvet^e ; Carme Calvis^f ; Ramó ; n Messeguer^f ; Concepció ; n Ló ; pez^a ; ^{conchi.lopez@qi.ub.es}
• 关键词：Platinacycles ; Ferrocene derivatives ; Pyrazoles ; Crystal structures ; Antitumoral activity
• 刊名：Journal of Organometallic Chemistry
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：828
• 期：Complete
• 页码：122-132
• 全文大小：1523 K
• 卷排序：828

文摘

One trimetallic (3) and two dimetallic (4 and 5) new platinacycles derived from the hybrid ferrocene/pyrazole [1-{MeO(CH2)2}-3,5-Ph2-4-(CH2Fc)-(C3N2)] (1) are described. Compound 3 has two units of ligand 1, adopting two different binding modes [(κ2-C,N) and (κ1-N)]; while in the other two (4 and 5), pyrazole 1 acts as a bidentate (κ2-C,N) ligand. The three compounds with identical cycloplatinated core have markedly different cytotoxic activity in front of MCF7, MDA-MB231 and HCT116 cancer cell lines. Compound [Pt{(κ2-C,N)[1-[MeO(CH2)2]-3-(C6H4)-5-Ph-4-(CH2Fc)-(C3N2)]}X (PPh3)] with X = Cl− (4) was more potent than its analogue with X = NO2− (5) in MCF7, MDA-MB-231 and HCT116 cancer cell lines; but the trimetallic product 3 showed no activity in these cell lines. Compound 4 is seven times more cytotoxic than cisplatin in the HCT-116 (colon) cancer cell line.