A facile preparation and crystal structure of romipeptide A

J Antibiot (Tokyo). 2022 Jan;75(1):48-50. doi: 10.1038/s41429-021-00487-2. Epub 2021 Nov 26.

Abstract

A double disulfide tethering depsipeptide dimer, romipeptide A (1) was prepared by NaOH catalyzed dimerization of romidepsin. Its structure was determined by analysis of NMR and HR-ESI-MS data as well as single crystal X-ray diffraction. Bioassay results showed that 1 exhibited good cytotoxic activity against two tumor cell lines B16 and HCT116. This study reported the single crystal data of 1 for the first time. The facile preparation of 1 afforded enough amount for its further biological evaluations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibiotics, Antineoplastic / chemical synthesis*
  • Antibiotics, Antineoplastic / pharmacology
  • Cell Line, Tumor
  • Crystallography, X-Ray
  • Drug Screening Assays, Antitumor
  • HCT116 Cells
  • Humans
  • Magnetic Resonance Spectroscopy
  • Melanoma, Experimental / drug therapy
  • Molecular Structure
  • Spectrometry, Mass, Electrospray Ionization
  • X-Ray Diffraction

Substances

  • Antibiotics, Antineoplastic