Rosselli Sergio, Bruno Maurizio, Maggio Antonella, Bellone Gabriella, Chen Tzu-Hsuan, Bastow Kenneth F, Lee Kuo-Hsiung
Dipartimento di Chimica Organica, Università di Palermo, Viale delle Scienze, 90128 Palermo, Italy.
J Nat Prod. 2007 Mar;70(3):347-52. doi: 10.1021/np060504w.
Atractyligenin (1) and several synthetic derivatives were tested and found to be active against tumor cell replication. Compound 1 was readily converted to the 2,15-diketo (3) or 15-keto (4) derivatives, which contain an alpha,beta-unsaturated ketone. Compounds 3 and 4 showed significant cytotoxic activity against all six tested cancer cell lines and were most potent against 1A9 ovarian cancer cells with EC50 values of 0.2 and 0.3 microM, respectively. These two 1-analogues are promising lead compounds for further investigation.
苍术素（1）和几种合成衍生物经过测试，发现对肿瘤细胞复制具有活性。化合物1很容易转化为含有α,β-不饱和酮的2,15-二酮（3）或15-酮（4）衍生物。化合物3和4对所有六种测试的癌细胞系均显示出显著的细胞毒性活性，对1A9卵巢癌细胞的活性最强，EC50值分别为0.2和0.3微摩尔。这两种1-类似物是有前景的先导化合物，有待进一步研究。
