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Copper(II) Complexes with Mixed Heterocycle Ligands as Promising Antibacterial and Antitumor Species

机译:用混合杂环配体的铜(II)配合物作为有前途的抗菌和抗肿瘤物种

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摘要

Complexes with mixed ligands [Cu(N-N)2(pmtp)](ClO4)2 ((1) N-N: 2,2′-bipyridine; (2) L: 1,10-phenanthroline and pmpt: 5-phenyl-7-methyl-1,2,4-triazolo[1,5-a]pyrimidine) were synthesized and structurally and biologically characterized. Compound (1) crystallizes into space group Pa and (2) in P-1. Both complexes display an intermediate stereochemistry between the two five-coordinated ones. The biological tests indicated that the two compounds exhibited superoxide scavenging capacity, intercalative DNA properties, and metallonuclease activity. Tests on various cell systems indicated that the two complexes neither interfere with the proliferation of Saccharomyces cerevisiae or BJ healthy skin cells, nor cause hemolysis in the active concentration range. Nevertheless, the compounds showed antibacterial potential, with complex (2) being significantly more active than complex (1) against all tested bacterial strains, both in planktonic and biofilm growth state. Both complexes exhibited a very good activity against B16 melanoma cells, with a higher specificity being displayed by compound (1). Taken together, the results indicate that complexes (1) and (2) have specific biological relevance, with potential for the development of antitumor or antimicrobial drugs.
机译:配合物混合配体[Cu(NN)2(PMTP)](CLO 4)2((1)NN:2,2'-Bi吡啶;(2)L:1,10-菲林和PMPT:5-苯基-7-合成和在结构上合成甲基-1,2,4-三唑[1,5-A]嘧啶。化合物(1)在P-1中结晶到空间组Pa和(2)中。两个复合物在两个五协调的复合体之间显示中间立体化学。生物学试验表明,两种化合物表现出超氧化物清除能力,间隔性DNA性能和金属核酸酶活性。对各种细胞系统的测试表明,两种复合物既不会干扰酿酒酵母或BJ健康皮肤细胞的增殖,也不会引起活性浓度范围内的溶血。然而,化合物显示出抗菌电位,复合(2)比浮游生物和生物膜生长状态在所有测试的细菌菌株中显着更活跃(1)。两种复合物对B16黑素瘤细胞表现出非常好的活性,并通过化合物(1)显示较高的特异性。连同,结果表明复合物(1)和(2)具有特异性生物相关性,具有抗肿瘤或抗微生物药物的发育潜力。

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