Journal
CHEMMEDCHEM
Volume 15, Issue 1, Pages 125-135Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201900549
Keywords
cancer; nutrient deprivation; antiproliferation; dearomatization; dimerization
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Funding
- EPSRC (DTP studentship)
- Cancer Research at Bath (CR@B)
- Japanese Society for the Promotion of Science (JSPS Kakenhi) [16 K08319]
- Kobayashi International Scholarship Foundation
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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.
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