Research output: Chapter in Book/Report/Conference proceeding › Conference contribution › Research › peer-review
Inhibition of the DNA repair enzyme TDP1 by the resin acid derivatives as a new way to increase the efficiency of glioblastoma chemotherapy. / Kovaleva, Kseniya; Oleshko, Olga; Yarovaya, Olga et al.
Actual Problems of Organic Chemistry and Biotechnology, OCBT 2020: Proceedings of the International Scientific Conference. ed. / Vasiliy Bakulev; Elena Kovaleva; Tatiana Glukhareva; Tatiana Beryozkina; Yuri Schafran; Polina Lyubyakina; Olga Koptyaeva. American Institute of Physics Inc., 2022. 020036 (AIP Conference Proceedings; Vol. 2390).Research output: Chapter in Book/Report/Conference proceeding › Conference contribution › Research › peer-review
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TY - GEN
T1 - Inhibition of the DNA repair enzyme TDP1 by the resin acid derivatives as a new way to increase the efficiency of glioblastoma chemotherapy
AU - Kovaleva, Kseniya
AU - Oleshko, Olga
AU - Yarovaya, Olga
AU - Cheresiz, Sergey
AU - Zakharenko, Alexandra
AU - Ponomarev, Konstantin
AU - Lavrik, Olga
AU - Pokrovsky, Andrey
AU - Salakhutdinov, Nariman
N1 - Funding Information: This work was supported by a grant from the Russian Science Foundation 19-73-00051 and FSUS-2020-0035. Publisher Copyright: © 2022 Author(s).
PY - 2022/2/4
Y1 - 2022/2/4
N2 - A new class of tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors has been found among resin acid derivatives. Several novel bisureas derived from dehydroabietylamine (DHAm) were synthesized and tested for TDP1 inhibition. The synthesized compounds showed IC50 values in the range of 0.09 to 0.19 μM. Several compounds demonstrated the enhancement of cytotoxic activity of the alkylating agent, Lomustine, the chemotherapeutic drug used for the glioblastoma (GBM) treatment. The effect has been studied in two GBM cell lines U-87 and SNB19.
AB - A new class of tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors has been found among resin acid derivatives. Several novel bisureas derived from dehydroabietylamine (DHAm) were synthesized and tested for TDP1 inhibition. The synthesized compounds showed IC50 values in the range of 0.09 to 0.19 μM. Several compounds demonstrated the enhancement of cytotoxic activity of the alkylating agent, Lomustine, the chemotherapeutic drug used for the glioblastoma (GBM) treatment. The effect has been studied in two GBM cell lines U-87 and SNB19.
UR - http://www.scopus.com/inward/record.url?scp=85125633015&partnerID=8YFLogxK
UR - https://www.mendeley.com/catalogue/36de599e-0c6a-34ab-a1dc-99f014ec6054/
U2 - 10.1063/5.0069407
DO - 10.1063/5.0069407
M3 - Conference contribution
AN - SCOPUS:85125633015
T3 - AIP Conference Proceedings
BT - Actual Problems of Organic Chemistry and Biotechnology, OCBT 2020
A2 - Bakulev, Vasiliy
A2 - Kovaleva, Elena
A2 - Glukhareva, Tatiana
A2 - Beryozkina, Tatiana
A2 - Schafran, Yuri
A2 - Lyubyakina, Polina
A2 - Koptyaeva, Olga
PB - American Institute of Physics Inc.
T2 - 2020 International Scientific Conference on Actual Problems of Organic Chemistry and Biotechnology, OCBT 2020
Y2 - 18 November 2020 through 21 November 2020
ER -
ID: 35611780