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Neo-tanshionlactone was first isolated from Tanshen,the rhizome of Salvia miltiorrhizaBunge,as an anti-tumor agent with unique structure in 2004.Functional analysis showed that neo-tanshionlactone expresses selective antibreast cancer activity. Firstly, it was active againstbreast cancer cell line but also showed insignificant activity against other cell lines, like skincancer and prostate cancer, which implies potential targeted therapy against breast cancer.Secondly, it was active against both Estrogen Receptor positive (ER+) breast cancer cell lines(MCF-7 and ZR-75-1) and Human Epidermal Growth Factor Receptor 2 over-expressing breastcancer cell line (SK-BR-3, HER2+), but was inactive against two ER- cell lines (MDA MB-231,and HS 587-T). Compare with the ER antagonist, tamoxifen, nto-tanshionlactone showed 10-foldmore potent and 20-fold more selective against the ER+ cell lines. Because of its potent andunique activity, it was total synthesized and the structure activity relationship (SAR) study furtherconfirmed the selective antibreast cancer activity. Both ih vitro and ih vivo studies were carriedout and supported neo-tanshionlactone and its derivate can be further studied as clinical trialcandidate. However, its mechanism of action is complex since SK-BR-3 is ER- which means ithas distinct mechanism from tamoxifen and other existing antibreast cancer drugs. Clarification ofthe mechanism may provide novel target for breast cancer treatment and is undergoing in ourlaboratory.