volume 45 issue 6 pages 647-655

Effective Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 Based on Monoterpenoids as Potential Agents for Antitumor Therapy

A A Chepanova 1
N S Li Zhulanov 2, 3
A. S. Sukhikh 3, 4
A. Zafar 5
J Reynisson 6
A L Zakharenko 1
O D Zakharova 1
D.V. Korchagina 2
K P Volcho 2, 3
O I Lavrik 1, 3
Publication typeJournal Article
Publication date2019-11-01
scimago Q4
wos Q3
SJR0.267
CiteScore1.9
Impact factor1.7
ISSN10681620, 1608330X, 15739163
Organic Chemistry
Biochemistry
Abstract
Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is one of the important DNA repair enzymes responsible for the repair of DNA damage caused by anticancer drugs, such as topotecan. In this regard, enzyme activity is one of the possible causes of tumor resistance to chemotherapy, and the use of inhibitors of this enzyme is considered as a promising adjuvant therapy. We have obtained a number of new isomeric naphthyl derivatives of thiophenyl octahydro-2H-chromene, the structure of one of which is confirmed by X-ray structural analysis. Based on molecular modeling data, the structure of the ligand-Tdp1 complex has been proposed. All compounds obtained inhibit Tdp1 at a concentration of about 2 μM. Low toxicity of three compounds was shown, which makes them promising candidates for the development of accompanying cancer therapy.
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Chepanova A. A. et al. Effective Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 Based on Monoterpenoids as Potential Agents for Antitumor Therapy // Russian Journal of Bioorganic Chemistry. 2019. Vol. 45. No. 6. pp. 647-655.
GOST all authors (up to 50) Copy
Chepanova A. A., Li Zhulanov N. S., Sukhikh A. S., Zafar A., Reynisson J., Zakharenko A. L., Zakharova O. D., Korchagina D., Volcho K. P., Salakhutdinov N. F., Lavrik O. I. Effective Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 Based on Monoterpenoids as Potential Agents for Antitumor Therapy // Russian Journal of Bioorganic Chemistry. 2019. Vol. 45. No. 6. pp. 647-655.
RIS |
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RIS Copy
TY - JOUR
DO - 10.1134/s1068162019060104
UR - https://doi.org/10.1134/s1068162019060104
TI - Effective Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 Based on Monoterpenoids as Potential Agents for Antitumor Therapy
T2 - Russian Journal of Bioorganic Chemistry
AU - Chepanova, A A
AU - Li Zhulanov, N S
AU - Sukhikh, A. S.
AU - Zafar, A.
AU - Reynisson, J
AU - Zakharenko, A L
AU - Zakharova, O D
AU - Korchagina, D.V.
AU - Volcho, K P
AU - Salakhutdinov, N. F.
AU - Lavrik, O I
PY - 2019
DA - 2019/11/01
PB - Pleiades Publishing
SP - 647-655
IS - 6
VL - 45
SN - 1068-1620
SN - 1608-330X
SN - 1573-9163
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2019_Chepanova,
author = {A A Chepanova and N S Li Zhulanov and A. S. Sukhikh and A. Zafar and J Reynisson and A L Zakharenko and O D Zakharova and D.V. Korchagina and K P Volcho and N. F. Salakhutdinov and O I Lavrik},
title = {Effective Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 Based on Monoterpenoids as Potential Agents for Antitumor Therapy},
journal = {Russian Journal of Bioorganic Chemistry},
year = {2019},
volume = {45},
publisher = {Pleiades Publishing},
month = {nov},
url = {https://doi.org/10.1134/s1068162019060104},
number = {6},
pages = {647--655},
doi = {10.1134/s1068162019060104}
}
MLA
Cite this
MLA Copy
Chepanova, A. A., et al. “Effective Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 Based on Monoterpenoids as Potential Agents for Antitumor Therapy.” Russian Journal of Bioorganic Chemistry, vol. 45, no. 6, Nov. 2019, pp. 647-655. https://doi.org/10.1134/s1068162019060104.