Mesh : Animals Antineoplastic Agents / adverse effects chemistry pharmacology Bridged Bicyclo Compounds, Heterocyclic / adverse effects chemistry pharmacology Drug Design Humans Leukocytes / drug effects metabolism Neoplasms / drug therapy pathology Patents as Topic Phosphoprotein Phosphatases / antagonists & inhibitors

来  源:   DOI:10.1517/13543776.2011.629190   PDF(Sci-hub)

Abstract:
BACKGROUND: Norcantharidin (7-oxabicyclo [2.2.1] heptane-2,3-dicarboxylic anhydride) is the demethylated form of cantharidin. Norcantharidin not only has strong anticancer activity, but also eliminates most side-effects in the urinary system, does not cause myelosuppression and increases the number of white blood cells. With structural modification, norcantharidin analogues show potential anticancer activities.
METHODS: A comprehensive patent review of norcantharidin analogues from 2006 to 2010 is presented. Protein phosphatase 1, 2A, 2B and 5 inhibitors are described. The review summarizes the new compounds and lays the foundation for seeking more effective anticancer compounds.
CONCLUSIONS: Although norcantharidin has improved activity and toxicity, the effects routinely do not satisfy the current clinical need. Exploring better analogues is vital for changing the current situation, but norcantharidin is a good lead compound.
摘要:
暂无翻译
公众号