Screening of a library of natural derivatives for their virus entry inhibition activity using pseudotype systems shows bornyl ester derivatives containing saturated N-heterocycles exhibiting the highest antiviral activity.
Herein, for the first time the complexation ability of a homological series of triphenylphosphonium surfactants (TPPB-n) toward DNA decamers has been explored.
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.
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