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.
Xihong Wang  1 ,  Kenneth F Bastow ,  Chang-Ming Sun ,  Yun-Lian Lin ,  Hsi-Jung Yu ,  Ming-Jaw Don ,  Tian-Shung Wu ,  Seikou Nakamura ,  Kuo-Hsiung Lee
Affiliations
  • 1. Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, USA.
PMID: 15509181 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.