2-Cyano-3,10-dioxooleana-1,9(11)-dien-28-oic acid anhydride. A novel and highly potent anti-inflammatory and cytoprotective agent |
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Authors: | Tadashi Honda Eric M Padegimas Emilie David Chitra Sundararajan Karen T Liby Charlotte Williams Michael B Sporn Melean Visnick |
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Institution: | 1. Department of Chemistry, Dartmouth College, Hanover, NH 03755, USA;2. Department of Pharmacology and Toxicology, Dartmouth Medical School, Hanover, NH 03755, USA;3. Reata Pharmaceutical Inc., Dallas, TX 75063, USA |
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Abstract: | 2-Cyano-3,10-dioxooleana-1,9(11)-dien-28-oic acid anhydride (CDDO anhydride) has been synthesized, which is the first example of an oleanane triterpenoid anhydride. CDDO anhydride shows potency similar to or higher than the corresponding acid (CDDO) in various in vitro and in vivo assays related to inflammation and carcinogenesis. Notably, preliminary phamacokinetics studies show that CDDO anhydride levels are higher than CDDO levels in mouse tissues and blood. Further evaluation of CDDO anhydride is in progress. |
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