2. Academic Validation
  3. Design, synthesis, and anti-inflammatory activity both in vitro and in vivo of new betulinic acid analogues having an enone functionality in ring A

Design, synthesis, and anti-inflammatory activity both in vitro and in vivo of new betulinic acid analogues having an enone functionality in ring A

  • Bioorg Med Chem Lett. 2006 Dec 15;16(24):6306-9. doi: 10.1016/j.bmcl.2006.09.012.
Tadashi Honda 1,  Karen T Liby,  Xiaobo Su,  Chitra Sundararajan,  Yukiko Honda,  Nanjoo Suh,  Renee Risingsong,  Charlotte R Williams,  Darlene B Royce,  Michael B Sporn,  Gordon W Gribble
Affiliations

Affiliation

  • 1 Department of Chemistry, Dartmouth College, Hanover, NH 03755, USA. [email protected]
PMID: 16996735 DOI: 10.1016/j.bmcl.2006.09.012
Abstract

Fifteen new betulinic acid analogues were designed, synthesized, and tested for anti-inflammatory activity. Many of these analogues effectively suppress nitric oxide (NO) production in RAW cells stimulated with interferon-gamma. Analogue 10 is highly and orally active in vivo for induction of the anti-inflammatory and cytoprotective enzyme, heme oxygenase-1.

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