期刊
JOURNAL OF ORGANIC CHEMISTRY
卷 86, 期 23, 页码 16675-16683出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.1c01939
关键词
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资金
- NSFC [81473124]
- Chinese Ministry of Education 111 Project [BP0820034]
The study revealed that Huanglongmycin congener 14 exhibited stronger cytotoxicity against tested cancer cells, and highlighted the critical role of the C-7 ethyl group of 14 in its binding to the DNA-topoisomerase I complex.
Huanglongmycin (HLM) congeners G-N (7-14) were isolated from Streptomyces sp. CB09001. Among them, 10-12 possesses a tricyclic scaffold with benzene-fused pyran/pyrone, confirmed by X-ray single crystal diffraction analysis of 12. The structure-activity relationship study of 1, 13, and 14 revealed not only the stronger cytotoxicity of 14 against tested cancer cells but also the critical role of the C-7 ethyl group of 14 in its binding to the DNA-topoisomerase I complex.
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