Antitumor Agents. 239. Isolation, structure elucidation, total synthesis, and anti-breast cancer activity of neo-tanshinlactone from Salvia miltiorrhiza.
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.
Wang
Xihong
X
Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, USA.
Bastow
Kenneth F
KF
Sun
Chang-Ming
CM
Lin
Yun-Lian
YL
Yu
Hsi-Jung
HJ
Don
Ming-Jaw
MJ
Wu
Tian-Shung
TS
Nakamura
Seikou
S
Lee
Kuo-Hsiung
KH
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology*; D001943:Breast Neoplasms; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D005260:Female; D005663:Furans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D011753:Pyrones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000096:biosynthesis; D011960:Receptors, Estrogen / Q000096:biosynthesis; D027561:Salvia miltiorrhiza
D000972:Antineoplastic Agents, Phytogenic; D005663:Furans; D011753:Pyrones; D018719:Erb-b2 Receptor Tyrosine Kinases; D011960:Receptors, Estrogen; C494351:neotanshinlactone