带有碱性氨基侧链的取代菲：一类新型抗乳腺癌药物。
Substituted phenanthrenes with basic amino side chains: a new series of anti-breast cancer agents.
作者信息
Srivastava Ajay Kumar, Sharma Ramesh, Mishra Rajeev, Balapure Anil Kumar, Murthy Puvvada S R, Panda Gautam
机构信息
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow, UP, India.
出版信息
Bioorg Med Chem. 2006 Mar 1;14(5):1497-505. doi: 10.1016/j.bmc.2005.10.002. Epub 2005 Oct 24.
In the course of our search for new anti-breast cancer agents, substituted phenanthrenes with basic amino side chains were synthesized and some of them showed remarkable antiproliferative activity against ER +ve MCF-7 cell line with IC(50) in the range of 3.53-22.25 microM. One of the compounds 15 ca showed anti-breast cancer activity in 7,12-dimethylbenz[a]anthracene (DMBA) induced hormone-dependent mammary tumor in rat and the activity was comparable to that shown by tamoxifen.
在我们寻找新型抗乳腺癌药物的过程中，合成了带有碱性氨基侧链的取代菲，其中一些对雌激素受体阳性的MCF-7细胞系显示出显著的抗增殖活性，半数抑制浓度（IC50）在3.53 - 22.25微摩尔范围内。化合物15 ca在7,12-二甲基苯并[a]蒽（DMBA）诱导的大鼠激素依赖性乳腺肿瘤中显示出抗乳腺癌活性，其活性与他莫昔芬相当。
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