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. Epub 2019 Sep 6.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Microbial Sensitivity Tests
  • Micromonospora / chemistry*
  • Spectrum Analysis / methods

Substances

  • Anti-Bacterial Agents

Supplementary concepts

  • Micromonospora yangpuensis