2. Academic Validation
  3. Design and synthesis of novel pipernonaline derivatives as anti-austerity agents against human pancreatic cancer PANC-1 cells

Design and synthesis of novel pipernonaline derivatives as anti-austerity agents against human pancreatic cancer PANC-1 cells

  • Bioorg Med Chem. 2022 Oct 1:71:116963. doi: 10.1016/j.bmc.2022.116963.
Takuya Okada 1,  Yuri Chino 2,  Keita Yokoyama 3,  Yuki Fujihashi 4,  Nguyễn Duy Phan 4,  Juthamart Maneenet 4,  Lanke Prudhvi 3,  Suresh Awale 5,  Naoki Toyooka 6
Affiliations

Affiliations

  • 1 Graduate School of Pharma-Medical Sciences, University of Toyama, Toyama 930-8555, Japan; Graduate School of Science and Engineering, University of Toyama, Toyama 930-8555, Japan. Electronic address: tokada@eng.u-toyama.ac.jp.
  • 2 Graduate School of Pharma-Medical Sciences, University of Toyama, Toyama 930-8555, Japan.
  • 3 Graduate School of Science and Engineering, University of Toyama, Toyama 930-8555, Japan.
  • 4 Natural Drug Discovery Laboratory, Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan.
  • 5 Natural Drug Discovery Laboratory, Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan. Electronic address: suresh@inm.u-toyama.ac.jp.
  • 6 Graduate School of Pharma-Medical Sciences, University of Toyama, Toyama 930-8555, Japan; Graduate School of Science and Engineering, University of Toyama, Toyama 930-8555, Japan.
PMID: 35969895 DOI: 10.1016/j.bmc.2022.116963
Abstract

Pipernonaline (1), one of the components of the spice pepper, preferentially reduced the survival of human pancreatic Cancer PANC-1 cells under nutrient-deprived conditions witha PC50 value of 7.2 μM, suggesting that1couldpotentially lead to the development ofnew anticanceragents basedon theanti-austerity strategy. We have synthesized a total of 31 pipernonaline derivatives, revealing clear structure-activity relationships. Compound 9, which showed the strongest preferential cytotoxicity among synthesized derivatives, inhibited Akt activation and Cancer cell migration, making it an extremely promising candidate compound for new pancreatic Cancer agents based on the anti-austerity strategy.

Keywords

Anti-austerity strategy; Pancreatic cancer; Pipernonaline; Structure-activity relationship.

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