Abstract

A series of σ-aryl platinum complexes with the sterically hindered phenol group of the general formula RPt[PPh₃]₂X (R = 3,5-di-tert-butyl-4-hydroxyphenyl; X = Cl (I), diclofenac (II), aspirin (III), and OOCR (IV)) is synthesized and characterized by ¹H, ¹³C, and ³¹P NMR spectroscopy, IR spectroscopy, and elemental analysis. The molecular structure of compound I is determined by X-ray diffraction (XRD) (CIF file CCDC no. 2243100). The electron and hydrogen atom transfers are studied by spectrophotometry in the CUPRAC and DPPH tests. Complexes I, II, and IV are active reducing agents of Cu(II). The antioxidant activity is studied as the ability of the compounds to inhibit lipoxygenase (LOX-1B). Compound I is found to be an inhibitor of LOX-1B. The antiproliferative properties of the complexes are studied in vitro on the HCT-116, MCF-7, and A-549 cancer cells and WI-38 normal cells. The synthesized compounds have a lower antiproliferative activity than that of cisplatin.

中文翻译：

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双氯芬酸、阿司匹林和 2,6-二叔丁基苯酚片段的反式铂复合物：合成和生物活性

摘要

一系列带有空间位阻酚基的σ-芳基铂配合物，通式为RPt[PPh ₃ ] ₂ X（R=3,5-二叔丁基-4-羟基苯基；X=Cl( I )，双氯芬酸合成了( II )、阿司匹林 ( III ) 和 OOCR ( IV ))，并通过¹ H、¹³ C 和³¹ P NMR 光谱、IR 光谱和元素分析进行​​表征。化合物I的分子结构通过X射线衍射(XRD)确定(CIF文件CCDC no.2243100)。在 CUPRAC 和 DPPH 测试中通过分光光度法研究电子和氢原子转移。配合物I、II和IV是 Cu(II) 的活性还原剂。抗氧化活性被研究为化合物抑制脂氧合酶（LOX-1B）的能力。发现化合物I是 LOX-1B 的抑制剂。在 HCT-116、MCF-7 和 A-549 癌细胞以及 WI-38 正常细胞上体外研究了复合物的抗增殖特性。合成的化合物具有比顺铂更低的抗增殖活性。