Synthetic studies toward aza-ellipticine analogs and their potential uses as novel anti-cancer therapeutics


Ellipticine is an established anticancer chemotherapeutic, however, its current method of synthesis requires many steps. MUSC researchers have developed a method to obtain ellipticine analogs in one step by utilizing radiation and an acid catalysis. The ellipticine family represents a class of natural products that have been used to develop potential treatments for cancer, HIV, and malarial infection. Recent communications have described rapid access approaches toward quninone4 and aza5 analogs from a common indoline core. Using the MUSC protocol, an alkylated isatin can be derived to form an aza- ellipticine core. Analogs have been produced, and inventors are working to explore the compounds as potential anticancer drugs and look at their biological effects.


Overview: Ellipticine is a member of the pyrido[4,3-b] carbazole alkaloids that were first isolated in 1959. Ten years later, the biological profile of these alkaloids began to blossom as promising antitumor compounds of interest demonstrating growth inhibition of various experimental tumors like S-180, andenocarcinoma-755, Leukemia L-1210, and myeoblastic leukemia. Two of the mechanisms of action affiliated with ellipticine are inhibition of DNA topoisomerase II activity and DNA intercalation. As the biological relevance of these compounds continues, the synthetic community remains engaged towards developing new strategies for better drug candidates.


Applications: Drug development, cancer therapeutics, chemotherapy

Advantages: 1 step synthesis

Key Words: Ellipticine, cancer, chemotherapy, drug development

Inventors: Christopher Lindsey & Craig Beeson
Patent Status: US 15/307,966

MUSC-FRD Technology ID: P14103


Patent Information:
For Information, Contact:
Scott Davis
Sr Licensing Manager
MUSC Foundation for Research Development
Christopher Lindsey
Craig Beeson
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