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Role of Sulfonate Appendage in the Protein Binding Affinity of Half‐Sandwich Ruthenium(II)(η6‐p‐Cym) Complexes
European Journal of Inorganic Chemistry ( IF 2.2 ) Pub Date : 2020-01-15 , DOI: 10.1002/ejic.201901089
Ahmed M. Mansour 1 , Ola R. Shehab 1 , Krzysztof Radacki 2
Affiliation  

Mono‐ and binuclear benzimidazole based half‐sandwich organoruthenium(II) compounds; [Run(triazolateCOOCH3,COOCH3)n6p‐Cym)nL]0/+/2+ (n = 1, L = LCH2CH3 (7) and HLSO3H (8); n = 2, L = LDTP (9)) were synthesized by [3+2] free catalyzed cycloaddition reaction of azide complexes 46 with electron‐poor alkyne dimethyl acetylene dicarboxylate. In comparison with the parent [RunCln6p‐Cym)nL]0/+/2 complexes (13), the lysozyme binding affinity of the corresponding triazolate compounds 79 was investigated by electrospray ionization mass spectrometry. Complexes bearing benzimidazole ligand with an alkylated sulfonate side chain (2 and 8) are able to bind lysozyme noncovalently, which have not been clearly seen by other investigated Ru(II) complexes. The complexes were assessed for their potential antimicrobial activity against some representative microbes. Complex 9 exhibits antifungal activity against C. albicans (MIC = 24 nm) and C. neoformans (MIC = 12 nm), perfect blood compatibility as well as no toxicity to non‐malignant cell line (human embryonic kidney cells (HEK293).

中文翻译:

磺酸盐在半三明治钌(II)(η6-p-Cym)配合物的蛋白质结合亲和力中的作用

单核和双核苯并咪唑半三明治有机钌(II)化合物; 的[Ru Ñ(三唑COOCH 3,COOCH 3Ñ(η 6 - p -Cym)Ñ L] 0 / + / 2 +Ñ = 1,L = L CH 2 CH 37)和HL SO3H8); ñ = 2, L = L DTP9))是由合成[3 + 2]叠氮化物复合物的游离催化环加成反应4 - 6与贫电子炔二甲基乙炔二羧酸酯。与父母[Ru n ClÑ(η 6 - p -Cym)Ñ L] 0 / + / 2复合物(1 - 3),溶菌酶结合相应的三唑的亲和力的化合物7 - 9通过电喷雾电离质谱分析。带有苯并咪唑配体的烷基化磺酸盐侧链(28)的配合物能够非共价结合溶菌酶,其他研究过的Ru(II)配合物还没有清楚地观察到。评估复合物对某些代表性微生物的潜在抗微生物活性。配合物9表现出抗真菌活性白色念珠菌(MIC = 24 n m)和新孢梭菌(MIC = 12 n m),具有完美的血液相容性,并且对非恶性细胞系(人类胚胎肾细胞(HEK293))无毒性。
更新日期:2020-01-15
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