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March 17, 2007Journal of Medicinal ChemistryOpen Access

Novel Tricyclic Compounds Having Acetylene Groups at C-8a and Cyano Enones in Rings A and C: Highly Potent Anti-inflammatory and Cytoprotective Agents

Tadashi Honda Chitra Sundararajan Hidenori Yoshizawa Xiaobo Su Yukiko Honda Karen T. Liby Michael B. Sporn Gordon W. Gribble

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Abstract

Novel C-8a functionalized tricyclic compounds having cyano enones in rings A and C have been synthesized and biologically evaluated. Among them, compounds with acetylene groups at C-8a show extremely high potency in in vitro and in vivo bioassays for anti-inflammatory and cytoprotective activities. Both in vitro and in vivo potencies are markedly higher than those of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO), which is being evaluated as an anticancer drug in phase I clinical trials.

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Honda et al. (2007) studied this question.

synapsesocial.com/papers/6a9b2d7f9d7092273c39796c https://doi.org/10.1021/jm070141c

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