NDLI: Synthesis and structure of [(η<sup>6</sup>-p-cymene)Ru(2-anthracen-9-ylmethylene-N-ethylhydrazinecarbothioamide)Cl]Cl; biological evaluation, topoisomerase II inhibition and reaction with DNA and human serum albumin

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Synthesis and structure of [(η⁶-p-cymene)Ru(2-anthracen-9-ylmethylene-N-ethylhydrazinecarbothioamide)Cl]Cl; biological evaluation, topoisomerase II inhibition and reaction with DNA and human serum albumin

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Metallomics Vol - 3 Issue - 4

Metallomics Vol - 3 Issue - 3

Metallomics Vol - 3 Issue - 2

Metallomics Vol -2

Metallomics Vol -1

Synthesis and structure of [(η⁶-p-cymene)Ru(2-anthracen-9-ylmethylene-N-ethylhydrazinecarbothioamide)Cl]Cl; biological evaluation, topoisomerase II inhibition and reaction with DNA and human serum albumin

Content Provider	Royal Society of Chemistry (RSC)
Author	Woods, Jason Beckford, Floyd Didion, Jacob Gerasimchuk, Nikolay Seeram, Navindra P. Gonzalez-Sarrias, Antonio Thessing, Jeffrey
Copyright Year	2011
Abstract	We have synthesized and evaluated the biological properties of a compound of the type [η6-p-cymene)Ru(EtATSC)Cl]Cl (1) where EtATSC = 2-anthracen-9-ylmethylene-N-ethylhydrazinecarbothioamide, a thiosemicarbazone. The complex has been characterized by elemental analysis, spectroscopically (NMR, UV-Vis, and IR) and structurally by XRD. The in vitro anticancer activity of 1 has been evaluated against two human colon cancer cell lines. The IC50 value for activity against HCT-116 was 224 ± 7 μM and 205 ± 5 μM against the Caco-2 cell line. The proficiency of 1 as an antibacterial agent was also evaluated against six bacterial strains. The minimum inhibitory concentration for Bacillus cereus was determined to be 5 μM and for Enterococcus faecalis it was 20 μM. At the maximum concentration tested the complex showed no activity against the Gram-negative strains. The complex binds strongly to human serum albumin with a binding constant of 1.37 ± 0.02 M−1 at 308 K on a single binding site. It is also a strong binder to DNA with an apparent binding constant of 2.82 × 105 M−1 at 308 K. 1 shows very good activity as a catalytic inhibitor of human topoisomerase II at concentrations as low as 20 μM.
Starting Page	491
Ending Page	502
Page Count	12
File Format	HTM / HTML PDF
ISSN	17565901
Volume Number	3
Issue Number	5
Journal	Metallomics
DOI	10.1039/c1mt00003a
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Open
Subject Keyword	Enterococcus faecalis Human serum albumin P-Cymene Colorectal cancer Binding constant Enzyme inhibitor Excipient X-ray crystallography Caco-2 DNA IC50 Minimum inhibitory concentration Bacillus Topoisomerase Semicarbazone Nuclear magnetic resonance Gram-negative bacteria Cancer NCI-60
Content Type	Text
Resource Type	Article
Subject	Chemistry Medicine Metals and Alloys Biochemistry Biomaterials Biophysics

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Synthesis and structure of [(η6-p-cymene)Ru(2-anthracen-9-ylmethylene-N-ethylhydrazinecarbothioamide)Cl]Cl; biological evaluation, topoisomerase II inhibition and reaction with DNA and human serum albumin

Reaction of the Anticancer Organometallic Ruthenium Compound, [(η 6-p-Cymene)Ru(ATSC)Cl]PF6 with Human Serum Albumin

Synthesis and characterization of Ru(II) arene complexes, [Ru(η6-arene)(dppm)H]+ (η6-arene=benzene, p-cymene or hexamethylbenzene), [Ru(η6-arene)(py)3]2+ and [Ru(η6-arene)(py)2Cl]+

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Half-sandwich ruthenium-arene complexes with thiosemicarbazones: Synthesis and biological evaluation of [(η6-p-cymene)Ru(piperonal thiosemicarbazones)Cl]Cl complexes

Synthesis and unexpected reactivity of [Ru(η $^{6}$-cymene)Cl$_{2}$(PPh$_{2}$Cl)], leading to [Ru(η $^{6}$-cymene)Cl$_{2}$(PPh$_{2}$H)] and [Ru(η $^{6}$-cymene)Cl$_{ 2 }$(PPh$_{2}$OH)] complexes

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Synthesis and structure of [(η⁶-p-cymene)Ru(2-anthracen-9-ylmethylene-N-ethylhydrazinecarbothioamide)Cl]Cl; biological evaluation, topoisomerase II inhibition and reaction with DNA and human serum albumin

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Synthesis and structure of [(η6-p-cymene)Ru(2-anthracen-9-ylmethylene-N-ethylhydrazinecarbothioamide)Cl]Cl; biological evaluation, topoisomerase II inhibition and reaction with DNA and human serum albumin

Synthesis and structure of [(η⁶-p-cymene)Ru(2-anthracen-9-ylmethylene-N-ethylhydrazinecarbothioamide)Cl]Cl; biological evaluation, topoisomerase II inhibition and reaction with DNA and human serum albumin