Antimicrobial and Antitumor Activity of Enantiopure Pybox–Osmium Complexes. Issue 8 (9th February 2015)

• Record Type: Journal Article
• Authors: Menéndez‐Pedregal, Estefanía; Manteca, Ángel; Sánchez, Jesús; Díez, J.; Gamasa, M. Pilar; Lastra, Elena
• Is Part Of: European journal of inorganic chemistry. Issue 8(2015)
• Page Start: 1424
• Page End: 1432
• Publication Date: 2015-02-09
• Subjects: Medicinal chemistry -- Antitumor agents -- Antimicrobial activity -- Osmium­ -- Tridentate ligands; Chemistry, Inorganic -- Periodicals; Organometallic chemistry -- Periodicals; Bioinorganic chemistry -- Periodicals; Solid state chemistry -- Periodicals; 546
• DOI: 10.1002/ejic.201403173
• Languages: English
• ISSNs: 1434-1948

Abstract

Abstract: 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 IC50 value of 2.7 ± 0.3 μM has been found for trans ‐[OsCl2 {( S, S )‐ i Pr‐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. Abstract : The antiproliferative activities of new water‐soluble osmium(II) complexes against microbes and tumor cell lines are studied. The IC50 value for trans ‐[OsCl2 {( S, S )‐ i Pr‐pybox}(1‐PhCH2 ‐PTA)][Br] {( S, S )‐ i Pr‐pybox = 2, 6‐bis[4′( S )‐isopropyloxazolin‐2′‐yl]pyridine, PTA = 1, 3, 5‐triaza‐7‐phosphatricyclo[3.3.1.1 3, 7 ]decane} against HeLa cells is 2.7 ± 0.3 μM .