Abstract

In this study, 1-(4-(trifluoromethyl)benzyl)-1H-imidazole, (ImCF₃) and 2,2′-bipyridyl, (bipy) ligands coordinating copper(II) complex have been synthesized and successfully characterized by single crystal X-ray diffraction, FT-IR and UV-vis and elemental analysis techniques. The agreement between experimental and theoretical results have been observed. Information about local and global chemical activity, electrophilic and nucleophilic nature of copper(II) complex have been theoretically obtained. The anti-angiogenic activity results indicated that copper(II) complex showed significantly very strong anti-angiogenic potential with higher anti-angiogenic score (average score = 1.06 ± 0.01) than the standard anti-angiogenic (±)-Thalidomide (average score = 0.8 ± 0.2) with no irritation and embryotoxicity whereas both ligands of the complex showed weak anti-angiogenic effects and one of the ligands ImCF₃ showed significant and higher irritation potential (86 ± 20%) when compared with the standard irritant agent SDS (84 ± 10%) on the CAM at 50 µg/pellet.

摘要

在这项研究中，1-(4-(三氟甲基)苄基)-1H-咪唑，(ImCF ₃) 和 2,2'-联吡啶基 (bipy) 配体配位铜 (II) 配合物已被合成，并通过单晶 X 射线衍射、FT-IR 和 UV-vis 以及元素分析技术成功表征。已经观察到实验结果和理论结果之间的一致性。理论上已经获得了关于铜（II）配合物的局部和全局化学活性、亲电和亲核性质的信息。抗血管生成活性结果表明，铜 (II) 复合物显示出非常强的抗血管生成潜力，抗血管生成评分（平均评分 = 1.06 ± 0.01）高于标准抗血管生成（±）-沙利度胺（平均评分 = 0.8 ± 0.2) 无刺激性和胚胎毒性，而复合物的两种配体均显示出较弱的抗血管生成作用，其中一种配体 ImCF_{与 CAM 上 50 µg/丸的标准刺激剂 SDS (84 ± 10%) 相比，图3}显示出显着和更高的刺激潜力 (86 ± 20%)。