volume 58 issue 24 pages 9522-9534

Synthesis and Characterization of 4,11-Diaminoanthra[2,3-b]furan-5,10-diones: Tumor Cell Apoptosis through tNOX-Modulated NAD+/NADH Ratio and SIRT1

Yi-Hui Lee 3
Yi-Ann Chen 3
Chia An Yeh 3
Lyubov G Dezhenkova 1
Valeria A. Glazunova 4
Jan Balzarini 5
Maria N Preobrazhenskaya 1
Pin-Ju Chueh 3, 7, 8, 9
Publication typeJournal Article
Publication date2015-12-15
scimago Q1
wos Q1
SJR1.801
CiteScore11.5
Impact factor6.8
ISSN00222623, 15204804
Drug Discovery
Molecular Medicine
Abstract
A series of new 4,11-diaminoanthra[2,3-b]furan-5,10-dione derivatives with different side chains were synthesized. Selected 2-unsubstituted derivatives 11-14 showed high antiproliferative potency on a panel of mammalian tumor cell lines including multidrug resistance variants. Compounds 11-14 utilized multiple mechanisms of cytotoxicity including inhibition of Top1/Top2-mediated DNA relaxation, reduced NAD(+)/NADH ratio through tNOX inhibition, suppression of a NAD(+)-dependent sirtuin 1 (SIRT1) deacetylase activity, and activation of caspase-mediated apoptosis. Here, for the first time, we report that tumor-associated NADH oxidase (tNOX) and SIRT1 are important cellular targets of antitumor anthracene-9,10-diones.
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GOST Copy
Tikhomirov A. S. et al. Synthesis and Characterization of 4,11-Diaminoanthra[2,3-b]furan-5,10-diones: Tumor Cell Apoptosis through tNOX-Modulated NAD+/NADH Ratio and SIRT1 // Journal of Medicinal Chemistry. 2015. Vol. 58. No. 24. pp. 9522-9534.
GOST all authors (up to 50) Copy
Tikhomirov A. S., Shchekotikhin A., Lee Y., Chen Y., Yeh C. A., Tatarskiy V., Dezhenkova L. G., Glazunova V. A., Balzarini J., Shtil A. A., Preobrazhenskaya M. N., Chueh P. Synthesis and Characterization of 4,11-Diaminoanthra[2,3-b]furan-5,10-diones: Tumor Cell Apoptosis through tNOX-Modulated NAD+/NADH Ratio and SIRT1 // Journal of Medicinal Chemistry. 2015. Vol. 58. No. 24. pp. 9522-9534.
RIS |
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RIS Copy
TY - JOUR
DO - 10.1021/acs.jmedchem.5b00859
UR - https://doi.org/10.1021/acs.jmedchem.5b00859
TI - Synthesis and Characterization of 4,11-Diaminoanthra[2,3-b]furan-5,10-diones: Tumor Cell Apoptosis through tNOX-Modulated NAD+/NADH Ratio and SIRT1
T2 - Journal of Medicinal Chemistry
AU - Tikhomirov, Alexander S
AU - Shchekotikhin, Andrey
AU - Lee, Yi-Hui
AU - Chen, Yi-Ann
AU - Yeh, Chia An
AU - Tatarskiy, Victor
AU - Dezhenkova, Lyubov G
AU - Glazunova, Valeria A.
AU - Balzarini, Jan
AU - Shtil, Alexander A.
AU - Preobrazhenskaya, Maria N
AU - Chueh, Pin-Ju
PY - 2015
DA - 2015/12/15
PB - American Chemical Society (ACS)
SP - 9522-9534
IS - 24
VL - 58
PMID - 26633734
SN - 0022-2623
SN - 1520-4804
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2015_Tikhomirov,
author = {Alexander S Tikhomirov and Andrey Shchekotikhin and Yi-Hui Lee and Yi-Ann Chen and Chia An Yeh and Victor Tatarskiy and Lyubov G Dezhenkova and Valeria A. Glazunova and Jan Balzarini and Alexander A. Shtil and Maria N Preobrazhenskaya and Pin-Ju Chueh},
title = {Synthesis and Characterization of 4,11-Diaminoanthra[2,3-b]furan-5,10-diones: Tumor Cell Apoptosis through tNOX-Modulated NAD+/NADH Ratio and SIRT1},
journal = {Journal of Medicinal Chemistry},
year = {2015},
volume = {58},
publisher = {American Chemical Society (ACS)},
month = {dec},
url = {https://doi.org/10.1021/acs.jmedchem.5b00859},
number = {24},
pages = {9522--9534},
doi = {10.1021/acs.jmedchem.5b00859}
}
MLA
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MLA Copy
Tikhomirov, Alexander S., et al. “Synthesis and Characterization of 4,11-Diaminoanthra[2,3-b]furan-5,10-diones: Tumor Cell Apoptosis through tNOX-Modulated NAD+/NADH Ratio and SIRT1.” Journal of Medicinal Chemistry, vol. 58, no. 24, Dec. 2015, pp. 9522-9534. https://doi.org/10.1021/acs.jmedchem.5b00859.