Journal
JOURNAL OF NATURAL PRODUCTS
Volume 79, Issue 11, Pages 2961-2967Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.6b00979
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Funding
- Ministry of Education and Science of Russian Federation [RFME-FI60414X0018]
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Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a repair enzyme for stalled DNA-topoisomerase 1 (Topl) cleavage complexes and other 3'-end DNA lesions. TDP1 is a perspective target for anticancer therapy based on Topl-poison-mediated DNA damage. Several novel usnic acid derivatives with an enamine moiety have been synthesized and tested as inhibitors of TDP1. The enamines of usnic acid showed IC50 values in the range of 0.16 to 2.0 mu M. These compounds revealed moderate cytotoxicity against human tumor MCF-7 cells. These new compounds enhanced the cytotoxicity of the established Topl poison camptothecin by an order of magnitude.
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