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Trioxacarcins and analogs: DNA-modifying compounds with potent anti-proliferative effects

The trioxacarcins are a new class of DNA-modifying natural products with potent antiproliferative effects (with subnanmolar IC70 values against lung, mammary, and CNS cancer cell lines). Trioxacarcin A, B, and C were first discovered and isolated from the culture broth of Streptomyces bottropensis and were shown to possess anti-tumor activity in murine models as well as antimicrobial activities (e.g., antibacterial, anti-fungal, anti-malarial activities). Fewer than a dozen trioxacarcins have been identified to date. The Myers laboratory has recently completed the first synthesis of a trioxacarcin, DC-45-A2, using a highly modular, convergent route that can serve as a highly diversifiable platform for the synthesis of trioxacarcins and analogs that are previously not available from natural sources or semi-synthetic approaches.

The novel synthetic route will be useful in exploring the biological and chemical activities of trioxacarcins and analogs in cancers and infectious diseases. Analogs of trioxacarcins may also be used as research tools to modify DNA.

Intellectual Property Status: Patent(s) Pending

Applications

In 2010, there are an estimated 24.6 million people in the world living with cancer. Cancer is responsible for 25% of all deaths in the United States and 13% worldwide. Sales of cytotoxic therapies for cancer reached $14 billion in 2009 across the seven major pharmaceutical markets.

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