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Antimicrobial and Antitumor Activity of Enantiopure Pybox–Osmium Complexes
Author(s) -
MenéndezPedregal Estefanía,
Manteca Ángel,
Sánchez Jesús,
Díez J.,
Gamasa M. Pilar,
Lastra Elena
Publication year - 2015
Publication title -
european journal of inorganic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.667
H-Index - 136
eISSN - 1099-0682
pISSN - 1434-1948
DOI - 10.1002/ejic.201403173
Subject(s) - chemistry , osmium , hela , enantiopure drug , dna , in vitro , stereochemistry , pyridine , apoptosis , cell culture , in vivo , antimicrobial , combinatorial chemistry , biochemistry , medicinal chemistry , organic chemistry , ruthenium , enantioselective synthesis , catalysis , genetics , biology
The antiproliferative activities of enantiopure ( S , S )‐ i Pr‐pybox osmium(II) complexes {( S , S )‐ i Pr‐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 IC 50 value of 2.7 ± 0.3 μ M has been found for trans ‐[OsCl 2 {( S , S )‐ i Pr‐pybox}(1‐PhCH 2 ‐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.