Research output: Contribution to journal › Article › peer-review
Dehydroabietylamine Ureas and Thioureas as Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Enhance the Antitumor Effect of Temozolomide on Glioblastoma Cells. / Kovaleva, Kseniya; Oleshko, Olga; Mamontova, Evgeniya et al.
In: Journal of Natural Products, Vol. 82, No. 9, 27.09.2019, p. 2443-2450.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - Dehydroabietylamine Ureas and Thioureas as Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Enhance the Antitumor Effect of Temozolomide on Glioblastoma Cells
AU - Kovaleva, Kseniya
AU - Oleshko, Olga
AU - Mamontova, Evgeniya
AU - Yarovaya, Olga
AU - Zakharova, Olga
AU - Zakharenko, Alexandra
AU - Kononova, Alena
AU - Dyrkheeva, Nadezhda
AU - Cheresiz, Sergey
AU - Pokrovsky, Andrey
AU - Lavrik, Olga
AU - Salakhutdinov, Nariman
N1 - Publisher Copyright: Copyright © 2019 American Chemical Society and American Society of Pharmacognosy.
PY - 2019/9/27
Y1 - 2019/9/27
N2 - A new class of tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors was found among resin acid derivatives. Several novel ureas and thioureas derived from dehydroabietylamine were synthesized and tested for TDP1 inhibition. The synthesized compounds showed IC50 values in the range of 0.1 to 3.7 μM and demonstrated low cytotoxicity against the human tumor cell lines U-937, U-87MG, MDA-MB, SK-Mel8, A-549, MCF7, T98G, and SNB19. Several compounds showed enhancement of the cytotoxic activity of the alkylating agent temozolomide, which is used as a first line therapy against glioblastoma (GBM), in the GBM cell lines U-87MG and SNB19.
AB - A new class of tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors was found among resin acid derivatives. Several novel ureas and thioureas derived from dehydroabietylamine were synthesized and tested for TDP1 inhibition. The synthesized compounds showed IC50 values in the range of 0.1 to 3.7 μM and demonstrated low cytotoxicity against the human tumor cell lines U-937, U-87MG, MDA-MB, SK-Mel8, A-549, MCF7, T98G, and SNB19. Several compounds showed enhancement of the cytotoxic activity of the alkylating agent temozolomide, which is used as a first line therapy against glioblastoma (GBM), in the GBM cell lines U-87MG and SNB19.
KW - TOPOISOMERASE-I
KW - TDP1
KW - DERIVATIVES
KW - KETONES
KW - ENZYME
KW - DAMAGE
UR - http://www.scopus.com/inward/record.url?scp=85071862995&partnerID=8YFLogxK
U2 - 10.1021/acs.jnatprod.8b01095
DO - 10.1021/acs.jnatprod.8b01095
M3 - Article
C2 - 31430155
AN - SCOPUS:85071862995
VL - 82
SP - 2443
EP - 2450
JO - Journal of Natural Products
JF - Journal of Natural Products
SN - 0163-3864
IS - 9
ER -
ID: 21465508