Antimicrobial and Antitumor Activity of Enantiopure Pybox-Osmium Complexes

作者：Menendez Pedregal Estefania; Manteca Angel; Sanchez Jesus; Diez J; Pilar Gamasa M; Lastra Elena

来源：European Journal of Inorganic Chemistry, 2015, 2015(8): 1424-1432.

DOI：10.1002/ejic.201403173

• Medicinal chemistry
• Antitumor agents
• Antimicrobial activity
• Osmium
• Tridentate ligands

The antiproliferative activities of enantiopure (S,S)-iPr-pybox osmium(II) complexes {(S,S)-iPr-pybox = 2,6-bis[4(S)-isopropyloxazolin-2-yl]pyridine} against microbes and tumor cell lines (HeLa and HT29) as well as their interactions with plasmidic DNA have been studied. All of the analyzed compounds interacted in vitro with plasmidic DNA. They also interacted in vivo with microbes and tumor cell lines, as demonstrated by their interference with microbial growth and induction of apoptosis in HeLa cells. In particular, an IC50 value of 2.7 +/- 0.3 M has been found for trans-[OsCl2{(S,S)-iPr-pybox}(1-PhCH2-PTA)][Br] (PTA = 1,3,5-triaza-7-phosphatricyclo[3.3.1.1(3,7)]decane). All of the water-soluble complexes used in these studies have been synthesized in high yields and were fully characterized.

• 出版日期2015-3