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Synthesis and antitumor activity of novel alkynyl (phosphine) digold(I) complexes
Transition Metal Chemistry ( IF 1.7 ) Pub Date : 2021-06-21 , DOI: 10.1007/s11243-021-00467-3
Qiu Mei Chen , Yi Chen , Xiang Hua Wu

A series of 1,4-disubstituted digold–alkynyl complexes, [(PPh3)Au]2(μ-C≡CAr–CH≡C)], in which the 1,4-diethenylbenzene bridge contains two alkyl or oligo(ethylene glycol)methylether side chains at different positions (2,5- and 2,3-positions), have been synthesized and structurally characterized by spectroscopic techniques. The structure of [(AuPPh3)2{µ-C≡C–C6H2(OC6H13)2-2,5-C≡C}] (2c) has been established by X-ray crystallography. Their antitumor activities in vitro were investigated by MTT assay against four tumor cell lines. Compared to alkyl-functionalized complexes, the oligo(ethylene glycol)methylether-functionalized complexes showed significant antitumor activity, which may be attributed to the improvement of the hydrophilicity of the complex to achieve the appropriate lipophilicity. In particular, complex [(AuPPh3)2{µ-C≡C–C6H2(OCH2CH2OCH2CH2OCH3)2-2,3-C≡C}] (2j) displayed high activity against the A549 cell line and low cytotoxicity toward normal cell lines. Notably, further investigations are required if complex 2j is to undergo trials as a new potential antitumor agent.



中文翻译:

新型炔基(膦)二金(I)配合物的合成及抗肿瘤活性

一系列 1,4-二取代二金-炔基配合物 [(PPh 3 )Au] 2 ( μ -C≡C Ar-CH≡C)],其中 1,4-二乙烯基苯桥包含两个烷基或寡聚不同位置(2,5-和2,3-位)的(乙二醇)甲基醚侧链已被合成并通过光谱技术进行结构表征。[(AuPPh 3 ) 2 {µ-C≡C–C 6 H 2 (OC 6 H 13 ) 2 -2,5-C≡C}] ( 2c) 已通过 X 射线晶体学确定。通过对四种肿瘤细胞系的 MTT 测定研究了它们的体外抗肿瘤活性。与烷基官能化配合物相比,低聚(乙二醇)甲基醚官能化配合物显示出显着的抗肿瘤活性,这可能是由于提高了配合物的亲水性以达到适当的亲脂性。特别地,络合物 [(AuPPh 3 ) 2 {µ-C≡C–C 6 H 2 (OCH 2 CH 2 OCH 2 CH 2 OCH 3 ) 2 -2,3-C≡C}] ( 2j) 对 A549 细胞系显示出高活性,对正常细胞系显示出低细胞毒性。值得注意的是,如果将复合物2j作为一种新的潜在抗肿瘤剂进行试验,则需要进一步研究。

更新日期:2021-06-21
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