Novel Tricyclic Compounds Having Acetylene Groups at C-8a and Cyano Enones in Rings A and C: Highly Potent Anti-inflammatory and Cytoprotective Agents
| Autor: | Karen T. Liby, Xiaobo Su, Yukiko Honda, Hidenori Yoshizawa, Michael B. Sporn, Tadashi Honda, Gordon W. Gribble, Chitra Sundararajan |
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| Rok vydání: | 2007 |
| Předmět: |
Male
Nitrile medicine.drug_class Stereochemistry Antineoplastic Agents Stereoisomerism Nitric Oxide Article Anti-inflammatory Cell Line Interferon-gamma Mice Structure-Activity Relationship chemistry.chemical_compound In vivo Nitriles Drug Discovery medicine Animals Structure–activity relationship Oleanolic Acid chemistry.chemical_classification Macrophages Anti-Inflammatory Agents Non-Steroidal Macrophage Activation In vitro chemistry Cytoprotection Alkynes Molecular Medicine Enantiomer Heterocyclic Compounds 3-Ring Tricyclic |
| Zdroj: | Journal of Medicinal Chemistry. 50:1731-1734 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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