Journal
ORGANIC LETTERS
Volume 10, Issue 15, Pages 3331-3334Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol801235h
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Funding
- NCI NIH HHS [R37 CA031845-28, R01 CA031845, CA31845, R37 CA031845] Funding Source: Medline
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The first series of systematically varied C7-functionalized bryostatin analogs (12 members in all) have been synthesized through an efficient and convergent route. A new hotspot for PKC affinity, not present in the natural products, has been discovered, allowing for affinity control and potentially for selective regulation of PKC isozymes. Several analogs exhibit single-digit nanomolar affinity to PKC and display superior activity compared to bryostatin against the leukemia cell line K562.
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