Title |
Cyclic Depsipeptide BE‐43547A2: Synthesis and Activity against Pancreatic Cancer Stem Cells
|
---|---|
Published in |
Angewandte Chemie. International Edition, October 2017
|
DOI | 10.1002/anie.201709744 |
Pubmed ID | |
Authors |
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 |
Abstract |
The asymmetric total synthesis of cyclic depsipeptide BE-43547A₂ was achieved in 15 linear steps on a 350 mg scale in one batch. Our synthesis is featured with highly diastereoselective construction of α-hydroxy-β-ketoamide via α-hydroxylation with a d.r. up to 86:1. BE-43547A₂ can significantly reduce the percentage of pancreatic cancer stem cells in Panc-1 cells, and dramatically ablate the tumorsphere forming capability of Panc-1 cells. The tumor-initiating assay in-vivo, a gold standard for cancer stem cell assays, confirmed BE-43547A₂ could abolish the tumorigenesis of Panc-1 cells. The anti-PCSC activity of BE-43547A₂ will make this depsipeptide scaffold a start for discovering new PCSC-targeting drug. |
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Country | Count | As % |
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United Kingdom | 2 | 25% |
Dominican Republic | 1 | 13% |
Germany | 1 | 13% |
Unknown | 4 | 50% |
Demographic breakdown
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Scientists | 3 | 38% |
Science communicators (journalists, bloggers, editors) | 2 | 25% |
Mendeley readers
Geographical breakdown
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Unknown | 16 | 100% |
Demographic breakdown
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Student > Bachelor | 2 | 13% |
Lecturer | 1 | 6% |
Student > Doctoral Student | 1 | 6% |
Other | 1 | 6% |
Other | 3 | 19% |
Unknown | 4 | 25% |
Readers by discipline | Count | As % |
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Biochemistry, Genetics and Molecular Biology | 1 | 6% |
Pharmacology, Toxicology and Pharmaceutical Science | 1 | 6% |
Social Sciences | 1 | 6% |
Mathematics | 1 | 6% |
Other | 0 | 0% |
Unknown | 3 | 19% |