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 with a PC50 value of 7.2 μM, suggesting that 1 could potentially lead to the development of new anticancer agents based on the anti-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.
Original language | English |
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Article number | 116963 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 71 |
DOIs | |
State | Published - 2022/10/01 |
Keywords
- Anti-austerity strategy
- Pancreatic cancer
- Pipernonaline
- Structure-activity relationship
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry