2. Academic Validation
  3. Yangpumicins F and G, Enediyne Congeners from Micromonospora yangpuensis DSM 45577

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

  • J Nat Prod. 2019 Sep 27;82(9):2483-2488. doi: 10.1021/acs.jnatprod.9b00229.
Zilong Wang 1,  Zhongqing Wen 1,  Ling Liu 1,  Xiangcheng Zhu 1 2,  Ben Shen,  Xiaohui Yan 1 3,  Yanwen Duan 1 2 3,  Yong Huang 1 3
Affiliations

Affiliations

  • 1 Xiangya International Academy of Translational Medicine at Central South University , Changsha , Hunan 410013 , People's Republic of China.
  • 2 Hunan Engineering Research Center of Combinatorial Biosynthesis and Natural Product Drug Discovery , Changsha , Hunan 410011 , People's Republic of China.
  • 3 National Engineering Research Center of Combinatorial Biosynthesis for Drug Discovery , Changsha , Hunan 410011 , People's Republic of China.
PMID: 31490685 DOI: 10.1021/acs.jnatprod.9b00229
Abstract

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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