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Small molecule inhibitors with antineoplastic and antiangiogenic activities

The molecule NAD+ is extensively utilized in cellular processes including cell signaling and respiration. The drug AP0866, a potent inhibitor of Nampt, the first and rate limiting enzyme of the mammalian NAD+ recycling pathway, is currently being tested in several Phase I and Phase I/II clinical trials against several forms of cancer. In the present invention, we have developed a new class of Nampt inhibitors. The concentration dependent activities of these agents have been tested in-vitro and directly compared with those of AP0866 against six human tumor cell lines including: breast, colon, glioma, prostate, pancreatic and lung cancer. Several of these agents demonstrate significantly higher activity than AP0866 in vitro, exhibiting significantly lower IC50 values, as well as higher cancer cell anti-proliferative effects.

-Anti-cancer therapy, diabetes, arthritis

-High potency against tumor cells
-Unique composition of matter

Additional Details


University of Missouri - Columbia

Intellectual Property Protection

Patent Issued

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