Antitumor Agents. 239. Isolation, structure elucidation, total synthesis, and anti-breast cancer activity of neo-tanshinlactone from Salvia miltiorrhiza

J Med Chem. 2004 Nov 4;47(23):5816-9. doi: 10.1021/jm040112r.

Abstract

Neo-tanshinlactone (1) was isolated and synthesized for the first time and evaluated in vitro against several human cancer cell lines. Compound 1 showed significant inhibition against two ER+ human breast cancer cell lines and was 10-fold more potent and 20-fold more selective as compared to tamoxifen citrate. Compound 1 also potently inhibited an ER-, HER-2 overexpressing breast cancer cell line. Therefore, this novel compound merits further development as an anti-breast cancer drug candidate.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemical synthesis
  • Antineoplastic Agents, Phytogenic / isolation & purification
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Breast Neoplasms
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Female
  • Furans / chemistry
  • Furans / isolation & purification
  • Furans / pharmacology*
  • Humans
  • Pyrones / chemistry
  • Pyrones / isolation & purification
  • Pyrones / pharmacology*
  • Receptor, ErbB-2 / biosynthesis
  • Receptors, Estrogen / biosynthesis
  • Salvia miltiorrhiza*

Substances

  • Antineoplastic Agents, Phytogenic
  • Furans
  • Pyrones
  • Receptors, Estrogen
  • neotanshinlactone
  • Receptor, ErbB-2