4.7 Article

Yangpumicins F and G, Enediyne Congeners from Micromonospora yangpuensis DSM 45577

期刊

JOURNAL OF NATURAL PRODUCTS
卷 82, 期 9, 页码 2483-2488

出版社

AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.9b00229

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资金

  1. NSFC [81473124, 81872779, 81530092]
  2. Chinese Ministry of Education 111 Project [B0803420]
  3. Fundamental Research Funds for the Central Universities of Central South University (CSU) [2018zzts878]
  4. NIH [GM115575]

向作者/读者索取更多资源

Enediyne natural products are among the most cytotoxic small molecules and thus excellent payload candidates for the development of antibody drug conjugates (ADCs). Here we report the isolation and structural elucidation of two new 10-membered anthraquinone-fused enediynes, yangpumicins (YPM) F (6) and G (7), together with five known congeners, YPM A-E (1-5), from Micromonospora yangpuensis DSM 45577. YPM F (6) and G (7) showed strong cytotoxicity against the tested human cancer cell lines, as well as activity against several Gram-positive and Gram-negative pathogens. The 1,2-diols in 6 and 7 promise to enable new linker chemistry for the development of YPM-based ADCs.

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