Sidechain Diversification of Grandifloracin Allows Identification of Analogues with Enhanced Anti-Austerity Activity against Human PANC-1 Pancreatic Cancer Cells

Benjamin E. Alexander, Sijia Sun, Matthew J. Palframan, Gabriele Kociok-Köhn, Dya Fita Dibwe, Shiro Watanabe, Lorenzo Caggiano*, Suresh Awale, Simon E. Lewis

*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

11 被引用数 (Scopus)

抄録

The natural product (+)-grandifloracin is a potent “anti-austerity” agent, able to suppress the ability of various pancreatic cancer cell lines to tolerate conditions of nutrient deprivation. Such anti-austerity agents represent a promising approach to cancer chemotherapy. Here we report the synthesis and biological evaluation of racemic analogues of grandifloracin bearing diverse sidechains, of which two show enhanced potency in comparison with the natural product. Additionally, several unexpected by-products containing modifications of the grandifloracin core were isolated, identified and similarly evaluated for biological activity.

本文言語英語
ページ(範囲)125-135
ページ数11
ジャーナルChemMedChem
15
1
DOI
出版ステータス出版済み - 2020/01/07

ASJC Scopus 主題領域

  • 創薬
  • 薬理学、毒性学および薬学一般
  • 分子医療
  • 生化学
  • 薬理学
  • 有機化学

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