Cyclic Depsipeptide BE-43547A2: Synthesis and Activity against Pancreatic Cancer Stem Cells

Yuanjun Sun, Yahui Ding, Dongmei Li, Ruifei Zhou, Xiuwen Su, Juan Yang, Xiaoqian Guo, Chuanke Chong, Jinghan Wang, Weicheng Zhang, Cuigai Bai, Liang Wang*, Yue Chen

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

23 Citations (Scopus)


Asymmetric total synthesis of the cyclic depsipeptide BE-43547A2 was achieved in 15 linear steps on a 350 mg scale in one batch. The synthesis features the highly diastereoselective construction of an α-hydroxy-β-ketoamide through α-hydroxylation with a d.r. of up to 86:1. BE-43547A2 significantly reduces the percentage of pancreatic cancer stem cells (PCSCs) in Panc-1 cell cultures, and dramatically reduces the tumorsphere-forming capability of Panc-1 cells. An in vivo tumor-initiation assay, a gold standard for cancer stem cell assays, confirmed that BE-43547A2 can abolish the tumorigenesis of Panc-1 cells. The anti-PCSC activity of BE-43547A2 could make this depsipeptide scaffold a promising starting point for discovering new PCSC-targeting drugs.

Original languageEnglish
Pages (from-to)14627-14631
Number of pages5
JournalAngewandte Chemie - International Edition
Issue number46
Publication statusPublished - 13 Nov 2017
Externally publishedYes


  • cancer stem cells
  • cyclic depsipeptides
  • hydroxylation
  • pancreatic cancer
  • total synthesis


Dive into the research topics of 'Cyclic Depsipeptide BE-43547A2: Synthesis and Activity against Pancreatic Cancer Stem Cells'. Together they form a unique fingerprint.

Cite this