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
  • 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.