Boron-based drugs are increasingly being investigated in many disease categories, with several pharmaceutical companies (e.g. GSK, Anacor (now Pfizer), and Takeda) dramatically expanding their boron research programs in recent years in the quest for novel drug candidates, e.g. Velcade® (bortezomib) which is used in the treatment of multiple myeloma. Almost all boron drugs investigated to date, however, are based upon boronic acids and boronate esters. In contrast, polyhedral boron clusters known as carboranes have rarely been exploited as new types of robust, structural frameworks in medicinal chemistry, and their use as enzyme inhibitors or receptor agonists/antagonists is largely underdeveloped. We are currently investigating the use of carboranes as unique frameworks in new drugs for the diagnosis and treatment of aggressive and intractable cancers such as malignant gliomas.
Current biological targets include: histone deacetylases (HDACs), indoleamine-2,3-dioxygenase 1 (IDO1), the 18 kDa Translocator protein (TSPO), and the P2X7 receptor.
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