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Novel TDP1 Inhibitors: Disubstituted Thiazolidine-2,4-Diones Containing Monoterpene Moieties. / Ivankin, Dmitry I; Kornienko, Tatyana E; Mikhailova, Marina A et al.

In: International Journal of Molecular Sciences, Vol. 24, No. 4, 3834, 14.02.2023.

Research output: Contribution to journal › Article › peer-review

Harvard

Ivankin, DI, Kornienko, TE, Mikhailova, MA, Dyrkheeva, NS, Zakharenko, AL, Achara, C, Reynisson, J, Golyshev, VM, Luzina, OA, Volcho, KP, Salakhutdinov, NF & Lavrik, OI 2023, 'Novel TDP1 Inhibitors: Disubstituted Thiazolidine-2,4-Diones Containing Monoterpene Moieties', International Journal of Molecular Sciences, vol. 24, no. 4, 3834. https://doi.org/10.3390/ijms24043834

APA

Ivankin, D. I., Kornienko, T. E., Mikhailova, M. A., Dyrkheeva, N. S., Zakharenko, A. L., Achara, C., Reynisson, J., Golyshev, V. M., Luzina, O. A., Volcho, K. P., Salakhutdinov, N. F., & Lavrik, O. I. (2023). Novel TDP1 Inhibitors: Disubstituted Thiazolidine-2,4-Diones Containing Monoterpene Moieties. International Journal of Molecular Sciences, 24(4), [3834]. https://doi.org/10.3390/ijms24043834

Vancouver

Ivankin DI, Kornienko TE, Mikhailova MA, Dyrkheeva NS, Zakharenko AL, Achara C et al. Novel TDP1 Inhibitors: Disubstituted Thiazolidine-2,4-Diones Containing Monoterpene Moieties. International Journal of Molecular Sciences. 2023 Feb 14;24(4):3834. doi: 10.3390/ijms24043834

Author

Ivankin, Dmitry I ; Kornienko, Tatyana E ; Mikhailova, Marina A et al. / Novel TDP1 Inhibitors: Disubstituted Thiazolidine-2,4-Diones Containing Monoterpene Moieties. In: International Journal of Molecular Sciences. 2023 ; Vol. 24, No. 4.

BibTeX

@article{8723368d3b06436e8c2690cd75013835,
title = "Novel TDP1 Inhibitors: Disubstituted Thiazolidine-2,4-Diones Containing Monoterpene Moieties",
abstract = "Tyrosyl-DNA-phosphodiesterase 1 (TDP1) is a promising target for antitumor therapy; the use of TDP1 inhibitors with a topoisomerase 1 poison such as topotecan is a potential combination therapy. In this work, a novel series of 3,5-disubstituted thiazolidine-2,4-diones was synthesized and tested against TDP1. The screening revealed some active compounds with IC50 values less than 5 μM. Interestingly, compounds 20d and 21d were the most active, with IC50 values in the submicromolar concentration range. None of the compounds showed cytotoxicity against HCT-116 (colon carcinoma) and MRC-5 (human lung fibroblasts) cell lines in the 1-100 μM concentration range. Finally, this class of compounds did not sensitize cancer cells to the cytotoxic effect of topotecan.",
keywords = "TDP1 inhibitors, thiazolidine-2,4-dione derivatives, tyrosyl-DNA-phosphodiesterase 1",
author = "Ivankin, {Dmitry I} and Kornienko, {Tatyana E} and Mikhailova, {Marina A} and Dyrkheeva, {Nadezhda S} and Zakharenko, {Alexandra L} and Chigozie Achara and J{\'o}hannes Reynisson and Golyshev, {Victor M} and Luzina, {Olga A} and Volcho, {Konstantin P} and Salakhutdinov, {Nariman F} and Lavrik, {Olga I}",
note = "Funding: The research was supported by the Russian Science Foundation (grant 19-13-00040).",
year = "2023",
month = feb,
day = "14",
doi = "10.3390/ijms24043834",
language = "English",
volume = "24",
journal = "International Journal of Molecular Sciences",
issn = "1661-6596",
publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",
number = "4",

}

RIS

TY - JOUR

T1 - Novel TDP1 Inhibitors: Disubstituted Thiazolidine-2,4-Diones Containing Monoterpene Moieties

AU - Ivankin, Dmitry I

AU - Kornienko, Tatyana E

AU - Mikhailova, Marina A

AU - Dyrkheeva, Nadezhda S

AU - Zakharenko, Alexandra L

AU - Achara, Chigozie

AU - Reynisson, Jóhannes

AU - Golyshev, Victor M

AU - Luzina, Olga A

AU - Volcho, Konstantin P

AU - Salakhutdinov, Nariman F

AU - Lavrik, Olga I

N1 - Funding: The research was supported by the Russian Science Foundation (grant 19-13-00040).

PY - 2023/2/14

Y1 - 2023/2/14

N2 - Tyrosyl-DNA-phosphodiesterase 1 (TDP1) is a promising target for antitumor therapy; the use of TDP1 inhibitors with a topoisomerase 1 poison such as topotecan is a potential combination therapy. In this work, a novel series of 3,5-disubstituted thiazolidine-2,4-diones was synthesized and tested against TDP1. The screening revealed some active compounds with IC50 values less than 5 μM. Interestingly, compounds 20d and 21d were the most active, with IC50 values in the submicromolar concentration range. None of the compounds showed cytotoxicity against HCT-116 (colon carcinoma) and MRC-5 (human lung fibroblasts) cell lines in the 1-100 μM concentration range. Finally, this class of compounds did not sensitize cancer cells to the cytotoxic effect of topotecan.

AB - Tyrosyl-DNA-phosphodiesterase 1 (TDP1) is a promising target for antitumor therapy; the use of TDP1 inhibitors with a topoisomerase 1 poison such as topotecan is a potential combination therapy. In this work, a novel series of 3,5-disubstituted thiazolidine-2,4-diones was synthesized and tested against TDP1. The screening revealed some active compounds with IC50 values less than 5 μM. Interestingly, compounds 20d and 21d were the most active, with IC50 values in the submicromolar concentration range. None of the compounds showed cytotoxicity against HCT-116 (colon carcinoma) and MRC-5 (human lung fibroblasts) cell lines in the 1-100 μM concentration range. Finally, this class of compounds did not sensitize cancer cells to the cytotoxic effect of topotecan.

KW - TDP1 inhibitors

KW - thiazolidine-2,4-dione derivatives

KW - tyrosyl-DNA-phosphodiesterase 1

UR - https://www.scopus.com/record/display.uri?eid=2-s2.0-85149019151&origin=inward&txGid=ad05da1248733206a7d6a185a7f5bbd4

UR - https://www.mendeley.com/catalogue/2f18e424-0c1e-3cad-bb69-2b9df0754b2c/

U2 - 10.3390/ijms24043834

DO - 10.3390/ijms24043834

M3 - Article

C2 - 36835244

VL - 24

JO - International Journal of Molecular Sciences

JF - International Journal of Molecular Sciences

SN - 1661-6596

IS - 4

M1 - 3834

ER -

ID: 44531124