2. Academic Validation
  3. Novel tricyclic compounds having acetylene groups at C-8a and cyano enones in rings A and C: highly potent anti-inflammatory and cytoprotective agents

Novel tricyclic compounds having acetylene groups at C-8a and cyano enones in rings A and C: highly potent anti-inflammatory and cytoprotective agents

  • J Med Chem. 2007 Apr 19;50(8):1731-4. doi: 10.1021/jm070141c.
Tadashi Honda 1,  Chitra Sundararajan,  Hidenori Yoshizawa,  Xiaobo Su,  Yukiko Honda,  Karen T Liby,  Michael B Sporn,  Gordon W Gribble
Affiliations

Affiliation

  • 1 Department of Chemistry, Dartmouth College, 6128 Burke Laboratory, Hanover, New Hampshire 03755, USA. th9@dartmouth.edu
PMID: 17367124 DOI: 10.1021/jm070141c
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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