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Download fileYangpumicins F and G, Enediyne Congeners from Micromonospora yangpuensis DSM 45577
journal contribution
posted on 2019-09-06, 15:35 authored by Zilong Wang, Zhongqing Wen, Ling Liu, Xiangcheng Zhu, Ben Shen, Xiaohui Yan, Yanwen Duan, Yong HuangEnediyne 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.