Dehydroabietylamine Ureas and Thioureas as Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Enhance the Antitumor Effect of Temozolomide on Glioblastoma Cells.

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ID: 12311
2019
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Abstract
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 IC 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.
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Authors Kovaleva, Kseniya;Oleshko, Olga;Mamontova, Evgeniya;Yarovaya, Olga;Zakharova, Olga;Zakharenko, Alexandra;Kononova, Alena;Dyrkheeva, Nadezhda;Cheresiz, Sergey;Pokrovsky, Andrey;Lavrik, Olga;Salakhutdinov, Nariman;
Journal Journal of natural products
Year 2019
DOI
10.1021/acs.jnatprod.8b01095
URL
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