Discovery of a DNA Topoisomerase I Inhibitor Huanglongmycin N and Its Congeners from Streptomyces sp. CB09001,The Journal of Organic Chemistry

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Discovery of a DNA Topoisomerase I Inhibitor Huanglongmycin N and Its Congeners from Streptomyces sp. CB09001
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2021-10-28 , DOI: 10.1021/acs.joc.1c01939
Saibin Zhu ₁ , Yeji Wang ₁ , Zhongqing Wen ₁ , Yanwen Duan _{1,

2,

3} , Yong Huang _{1,

3}

Affiliation

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.

中文翻译：

从链霉菌中发现 DNA 拓扑异构酶 I 抑制剂黄龙霉素 N 及其同系物。CB09001

黄龙霉素 (HLM) 同系物 G-N ( 7 - 14 ) 分离自链霉菌属。CB09001。其中，10 – 12具有苯稠合吡喃/吡喃酮的三环支架，经12的 X 射线单晶衍射分析证实。1、13和14的构效关系研究揭示了 14 不仅对测试的癌细胞具有更强的细胞毒性，而且还揭示了14的 C- 7乙基在其与 DNA-拓扑异构酶 I 复合物结合中的关键作用。

更新日期：2021-12-03

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