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

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journal contribution
posted on 06.09.2019, 15:35 authored by Zilong Wang, Zhongqing Wen, Ling Liu, Xiangcheng Zhu, Ben Shen, Xiaohui Yan, Yanwen Duan, Yong Huang
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 (15), 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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