Evaluation of synthetic coumarins for antiausterity cytotoxicity against pancreatic cancers

Conner M. Farley, Dya Fita Dibwe, Jun Ya Ueda, Eric A. Hall, Suresh Awale, Jakob Magolan*

*この論文の責任著者

研究成果: ジャーナルへの寄稿学術論文査読

23 被引用数 (Scopus)

抄録

A series of functionalized coumarins were synthesized and evaluated for their capacity to inhibit the resistance to starvation of pancreatic cancer cells. This form of cytotoxicity, termed 'antiausterity' activity, was evaluated using a preferential cytotoxicity assay that compared cell survival in nutrient poor and nutrient rich conditions. Six of the seventeen compounds showed weak antiausterity activity against PANC-1. Compound 34 was active against PANC-1, MIA PaCa-2, and Capan-1 cancer cell lines. All of the compounds tested were simplified structural analogs of previously reported natural product leads. Six of the compounds, including 34, contain functionalized triazoles as novel potential bioisosteres of the side chain of the natural product angelmarin. Overall, the analogs were found to have low antiausterity activity relative to the corresponding natural products.

本文言語英語
ページ(範囲)1471-1474
ページ数4
ジャーナルBioorganic and Medicinal Chemistry Letters
26
5
DOI
出版ステータス出版済み - 2016/03/01

ASJC Scopus 主題領域

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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