期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 60, 期 3, 页码 899-912出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00795
关键词
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资金
- DGAPA-UNAM
- CONACYT for the CONACyT-SNI grant
- [UNAM-PAIP 5000-9047]
- [UNAM- PAPIIT IG200616]
Three water-soluble Ru(II) chiral heteroleptic coordination compounds [Ru(en)(pdto)]Cl-2 (1), [110(gly)(pdto)]Cl (2),, and [Ru(acac)(pdto)]Cl (3), where pdto 2,2'-[1,2-ethanediylbis-(sulfanecliy1-2,1-ethanediyO]dipyridine, en = ethylendiamine, gly = glycinate, and acac = acetylacetonate, have been synthezised and fully characterized. The crystal structures of compounds 1-3 are described. The IC50 values for compounds 1-3 are within nanomolar range (14, 12, and 6 nM, respectively). The cytotoxicity for human peripheral blood lymphocytes is extremely low (>100 mu M). Selectivity indexes for Ru(II) compounds are in the range 700-1300. Trophozoites exposed to Ru(II) compounds die through an apoptotic pathway triggered by ROS production. The orally administration to infected mice induces a total elimination of the parasite charge in mice faeces 1-2-fold faster than metronidazole. Besides, all compounds inhibit the trophozoite proliferation in amoebic liver abscess induced in hamster. All our results lead us to propose these compounds as promising candidates as antiparasitic agents.
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