Applying a Trojan Horse Strategy to Ruthenium Complexes in the Pursuit of Novel Antibacterial Agents
作者:Quentin Laurent、Lucinda K. Batchelor、Paul J. Dyson
DOI:10.1021/acs.organomet.7b00885
日期:2018.3.26
Siderophores are iron chelators secreted by bacteria to scavenge iron(III) from their surrounding environment. They possess their own internalization pathway that is sufficiently unselective to be hijacked, making them suitable for Trojan Horse strategy applications. A commercially available siderophore, deferoxamine B (DFO), was derivatized at the primary amine with carboxylic acids bearing different
铁载体是细菌分泌的铁螯合剂,可从周围环境中清除铁(III)。他们拥有自己的内部化途径,该途径对于被劫持而言具有足够的选择性,因此非常适合特洛伊木马策略应用。将市售的铁载体去铁胺B(DFO)在伯胺上用带有不同配体的羧酸衍生化,以提供与钌的单和双齿配合物,以及RFOTA样配合物,其中DFO束缚在配位的芳烃环上。测试了这些化合物对关键ESKAPE病原体的抗菌活性,并对健康(HEK-293)和肿瘤(A2780)人类细胞进行了抗增殖研究。一些复合物显示出有趣的双重抗癌和抗菌特性。