Trithiolato-bridged dinuclear ruthenium(II)-arene conjugates tethered with lipophilic units: Synthesis and Toxoplasma gondii antiparasitic activity
نویسندگان
چکیده
Trithiolato-bridged dinuclear ruthenium(II)-arene complexes are active against various parasites including Toxoplasma gondii. Lipids, isoprenoids and lipoate metabolites scavenged by T. gondii from the host cell but also synthesized parasite, these molecules can be appended to diruthenium moiety in a conjugate approach aiming at compounds with improved antiparasitic activity selectivity. The synthesis vitro evaluation of 23 new trithiolato bearing lipophilic units reported. influence several structural elements as nature pendant type connecting bond between two on conjugates’ biological properties were examined. In primary screening, efficacy cytotoxicity assessed 0.1 1 µM transgenic tachyzoites constitutively expressing β-galactosidase human foreskin fibroblasts (HFF) cells. For 14 selected conjugates half-maximal inhibitory concentration (IC50) their effect HFF viability 2.5 determined. decanoic, oleic elaidic ester 13a, 16a 17a efficiently inhibited parasite proliferation (IC50 values 0.065, 0.127 0.123 µM, respectively) no deserve further attention.
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ژورنال
عنوان ژورنال: Journal of Organometallic Chemistry
سال: 2023
ISSN: ['1872-8561', '0022-328X']
DOI: https://doi.org/10.1016/j.jorganchem.2023.122624