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Synthesis, structure and in vitro anticancer activity of ruthenium(II) and platinum(II) complexes with chiral aminophosphine ligands
Transition Metal Chemistry ( IF 1.6 ) Pub Date : 2021-02-12 , DOI: 10.1007/s11243-020-00446-0
Ozlem Sari , Anna Schüttler , Peter Lönnecke , Patrick J. Bednarski , Evamarie Hey-Hawkins , Mehmet Karakus

(R)-[Ru(η6-p-MeC6H4iPr)Cl2{Ph2PNHCH(CH3)(C6H4-4-F)}] (1) and cis-(R,R)-[PtCl2{Ph2PNHCH(CH3)(C6H4-4-F)}2] (2) have been obtained by the reaction of the chiral aminophosphine (R)-Ph2PNHCH(CH3)(C6H4-4-F) with [{RuCl(μ-Cl)(η6-p-MeC6H4iPr)}2] or [PtCl2(cod)] (cod = cycloocta-1,5-diene). Both complexes were characterized by physico-chemical and spectroscopic methods. Compound 1 was also characterized by X-ray crystallography. The antitumor potential of both compounds was investigated by using the crystal violet antiproliferation assay. Complexes 1 and 2 were found to inhibit the growth of three human cancer cell lines, whereby the Ru complex was considerably more potent than the Pt complex, with IC50 values between 1 and 3 and 12–15 µM, respectively, but still less potent than cisplatin in the same three cell lines.



中文翻译:

具有手性氨基膦配体的钌(II)和铂(II)配合物的合成,结构和体外抗癌活性

- [R )- [茹(η 6 - p -MeC 6 ħ 4PR)氯2 {博士2 PNHCH(CH 3)(C 6 H ^ 4 -4-F)}](1)和顺式- (R, R)-[PtCl 2 {Ph 2 PNHCH(CH 3)(C 6 H 4 -4-F)} 2 ](2)通过手性氨基膦(R)-Ph 2 PNHCH(CH 3)反应制得。)(碳6 H 4-4-F)与[{的RuCl(μ-Cl)的(η 6 - p -MeC 6 ħ 4PR)} 2 ]或[氯铂酸2(COD)](COD =环辛-1,5-二烯)。两种配合物均通过物理化学和光谱法表征。化合物1还通过X射线晶体学表征。通过使用结晶紫抗增殖试验研究了这两种化合物的抗肿瘤潜力。发现复合物12抑制了三种人类癌细胞系的生长,因此Ru复合物比Pt复合物更有效,IC 50 值分别在1至3和12–15 µM之间,但在相同的三个细胞系中,其效价仍低于顺铂。

更新日期:2021-02-12
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