Open Access
Journal of Medicinal Chemistry, volume 58, issue 21, pages 8475-8490
Synthesis, Anticancer Activity, and Genome Profiling of Thiazolo Arene Ruthenium Complexes
Grozav Adriana
1
,
Balacescu Ovidiu
2
,
Bălăcescu Loredana
2
,
Cheminel Thomas
3
,
Neagoe Ioana Berindan
2, 4
,
Therrien Bruno
3
1
Faculty
of Pharmacy, “Iuliu Hatieganu” University of Medicine and Pharmacy, Victor Babes Str. 41, RO-400012 Cluj-Napoca, Romania
|
2
Department
of Functional Genomics, Proteomics and Experimental Pathology, The Oncology Institute “Prof Dr. Ion Chiricuta”, 34-36 Republicii Str, RO-400015, Cluj-Napoca, Romania
|
3
4
Research
Center of Functional Genomics, Biomedicine and Translational Medicine,
“Iuliu Hatieganu″ University of Medicine and Pharmacy, 23 Marinescu Str, RO-400337 Cluj-Napoca, Romania
|
Publication type: Journal Article
Publication date: 2015-10-30
Journal:
Journal of Medicinal Chemistry
Quartile SCImago
Q1
Quartile WOS
Q1
Impact factor: 7.3
ISSN: 00222623, 15204804
Drug Discovery
Molecular Medicine
Abstract
Sixteen hydrazinyl-thiazolo arene ruthenium complexes of the general formula [(η(6)-p-cymene)Ru(N,N'-hydrazinyl-thiazolo)Cl]Cl were synthesized. All complexes were tested in vitro for their antiproliferative activity on three tumor cell lines (HeLa, A2780, and A2780cisR) and on a noncancerous cell line (HFL-1). A superior cytotoxic activity of the ruthenium complexes as compared to cisplatin and oxaliplatin, on both cisplatin-sensitive and cisplatin resistant ovarian cancer cells, was observed. In addition, the biological activity of two selected derivatives was evaluated using microarray gene expression assay and ingenuity pathway analysis. p53 signaling was identified as an important pathway modulated by both arene ruthenium compounds. New activated molecules such as FAS, ZMAT3, PRMT2, BBC3/PUMA, and PDCD4, whose overexpressions are correlated with overcoming resistance to cisplatin therapy, were also identified as potential targets. Moreover, the arene ruthenium complexes can be used in association with cisplatin to prevent cisplatin resistance development and synergistically to induce cell death in ovarian cancer cells.
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Citations by publishers
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5 publications, 10.42%
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4 publications, 8.33%
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4 publications, 8.33%
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1 publication, 2.08%
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1 publication, 2.08%
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1 publication, 2.08%
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1 publication, 2.08%
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Proceedings of the National Academy of Sciences (PNAS)
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Proceedings of the National Academy of Sciences (PNAS)
1 publication, 2.08%
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2
4
6
8
10
12
14
16
18
20
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- We do not take into account publications that without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
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Grozav A. et al. Synthesis, Anticancer Activity, and Genome Profiling of Thiazolo Arene Ruthenium Complexes // Journal of Medicinal Chemistry. 2015. Vol. 58. No. 21. pp. 8475-8490.
GOST all authors (up to 50)
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Grozav A., Balacescu O., Bălăcescu L., Cheminel T., Neagoe I. B., Therrien B. Synthesis, Anticancer Activity, and Genome Profiling of Thiazolo Arene Ruthenium Complexes // Journal of Medicinal Chemistry. 2015. Vol. 58. No. 21. pp. 8475-8490.
Cite this
RIS
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TY - JOUR
DO - 10.1021/acs.jmedchem.5b00855
UR - https://doi.org/10.1021%2Facs.jmedchem.5b00855
TI - Synthesis, Anticancer Activity, and Genome Profiling of Thiazolo Arene Ruthenium Complexes
T2 - Journal of Medicinal Chemistry
AU - Grozav, Adriana
AU - Bălăcescu, Loredana
AU - Cheminel, Thomas
AU - Balacescu, Ovidiu
AU - Neagoe, Ioana Berindan
AU - Therrien, Bruno
PY - 2015
DA - 2015/10/30 00:00:00
PB - American Chemical Society (ACS)
SP - 8475-8490
IS - 21
VL - 58
SN - 0022-2623
SN - 1520-4804
ER -
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@article{2015_Grozav,
author = {Adriana Grozav and Loredana Bălăcescu and Thomas Cheminel and Ovidiu Balacescu and Ioana Berindan Neagoe and Bruno Therrien},
title = {Synthesis, Anticancer Activity, and Genome Profiling of Thiazolo Arene Ruthenium Complexes},
journal = {Journal of Medicinal Chemistry},
year = {2015},
volume = {58},
publisher = {American Chemical Society (ACS)},
month = {oct},
url = {https://doi.org/10.1021%2Facs.jmedchem.5b00855},
number = {21},
pages = {8475--8490},
doi = {10.1021/acs.jmedchem.5b00855}
}
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MLA
Copy
Grozav, Adriana, et al. “Synthesis, Anticancer Activity, and Genome Profiling of Thiazolo Arene Ruthenium Complexes.” Journal of Medicinal Chemistry, vol. 58, no. 21, Oct. 2015, pp. 8475-8490. https://doi.org/10.1021%2Facs.jmedchem.5b00855.