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水溶性铼膦配合物,包含 PhC(X) 基团(X = O,NH):结构和细胞毒性研究。

Water-Soluble Rhenium Phosphine Complexes Incorporating the PhC(X) Motif (X = O, NH): Structural and Cytotoxicity Studies.

机构信息

Department of Chemistry & Biochemistry , University of Hull , Cottingham Road , Hull HU6 7RX , U.K.

Department of Biomedical Sciences , University of Hull , Cottingham Road , Hull HU6 7RX , U.K.

出版信息

Inorg Chem. 2020 Feb 17;59(4):2367-2378. doi: 10.1021/acs.inorgchem.9b03239. Epub 2020 Jan 27.

Abstract

Reaction of [ReOCl(PPh)] or [ReOI(PPh)] with 2,2'-diphenylglycine (dpgH) in refluxing ethanol afforded the air-stable complex [ReO(dpgH)(dpg)(PPh)] (). Treatment of [ReO(OEt)I(PPh)] with 1,2,3-triaza-7-phosphaadamantane (PTA) afforded the complex [ReO(OEt)I(PTA)] (). Reaction of [ReOI(PTA)] with dpgH led to the isolation of the complex [Re(NCPh)I(PTA)]·0.5EtOH (·0.5EtOH). A similar reaction but using [ReOX(PTA)] (X = Cl, Br) resulted in the analogous halide complexes [Re(NCPh)Cl(PTA)]·2EtOH (·2EtOH) and [Re(NCPh)(PTA)Br]·1.6EtOH (·1.6EtOH). Using benzilic acid (2,2'-diphenylglycolic acid, benzH) with afforded the complex [ReO(benz)(PTA)][PTAH]·EtOH (·EtOH). The potential for the formation of complexes using radioisotopes with relatively short half-lives suitable for nuclear medicine applications by developing conditions for [Re(NCPh)(dpg)I(PTA)] ()[ReO] in a 4 h time scale was investigated. A procedure for the technetium analog of complex [Re(NCPh)I(PTA)] () from Tc[TcO] was then investigated. The molecular structures of - are reported; complexes - have been studied using in vitro cell assays (HeLa, HCT116, HT-29, and HEK 293) and were found to have IC values in the range of 29-1858 μM.

摘要

[ReOCl(PPh)] 或 [ReOI(PPh)] 与 2,2'-二苯甘氨酸(dpgH)在回流乙醇中反应,得到稳定的空气的配合物 ReO(dpgH)(dpg)(PPh)。用 1,2,3-三氮杂-7-磷杂金刚烷(PTA)处理 [ReO(OEt)I(PPh)] 得到配合物 ReO(OEt)I(PTA)。用 dpgH 处理 [ReOI(PTA)] 得到配合物 [Re(NCPh)I(PTA)]·0.5EtOH(·0.5EtOH)。类似的反应,但是使用 [ReOX(PTA)](X = Cl,Br)得到相应的卤化物配合物 [Re(NCPh)Cl(PTA)]·2EtOH(·2EtOH)和 [Re(NCPh)(PTA)Br]·1.6EtOH(·1.6EtOH)。用 2,2'-二苯乙醇酸(2,2'-二苯甘醇酸,benzH)与 反应,得到配合物 [ReO(benz)(PTA)][PTAH]·EtOH(·EtOH)。通过开发在 4 小时时间尺度内形成 Re(NCPh)(dpg)I(PTA)[ReO]的条件,研究了使用半衰期较短的放射性同位素形成配合物的可能性,这些同位素适合核医学应用。然后研究了从 Tc[TcO] 得到复合物 Re(NCPh)I(PTA)的锝类似物的程序。报道了 - 的分子结构;用体外细胞试验(HeLa、HCT116、HT-29 和 HEK 293)研究了配合物 -,发现它们的 IC 值在 29-1858 μM 范围内。

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