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

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.

• Authors: Xihong Wang, Kenneth F Bastow, Chang-Ming Sun, Yun-Lian Lin, Hsi-Jung Yu, Ming-Jaw Don, Tian-Shung Wu, Seikou Nakamura, Kuo-Hsiung Lee
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 47 Issue 23 Pg. 5816-9 (Nov 04 2004) ISSN: 0022-2623 [Print] United States
• PMID: 15509181 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)

Chemical References

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

Topics

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