Journal
ORGANIC LETTERS
Volume 17, Issue 18, Pages 4546-4549Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.5b02262
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- St. Mary's College of Maryland
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Combretastatin A4 is a stilbenoid tubulin binding mitotic inhibitor whose conformation greatly influences its potency, making it an excellent candidate for adaptation as a photoactivatable tool. Herein we report a novel synthesis, the facile isomerization with commercial grade equipment, and biological activity of azo-combretastatin A4 in vitro and in human cancer cells. Photoisomerized azo-combretestatin A4 is at least 200-fold more potent in cellular culture, making it a promising phototherapeutic and biomedical research tool.
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