| Literature DB >> 31430155 |
Kseniya Kovaleva1,2, Olga Oleshko2, Evgeniya Mamontova3, Olga Yarovaya1,2, Olga Zakharova3, Alexandra Zakharenko3, Alena Kononova2, Nadezhda Dyrkheeva3, Sergey Cheresiz2,4, Andrey Pokrovsky2, Olga Lavrik2,3, Nariman Salakhutdinov1,2.
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 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.Entities:
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Year: 2019 PMID: 31430155 DOI: 10.1021/acs.jnatprod.8b01095
Source DB: PubMed Journal: J Nat Prod ISSN: 0163-3864 Impact factor: 4.050