Ogawa Takumi, Ohta Kiminori, Yoshimi Tomohiro, Yamazaki Hiroto, Suzuki Tomoharu, Ohta Shigeru, Endo Yasuyuki
Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai 981-8558, Japan.
Bioorg Med Chem Lett. 2006 Aug 1;16(15):3943-6. doi: 10.1016/j.bmcl.2006.05.032. Epub 2006 Jun 2.
A series of m-carborane derivatives was prepared based upon the structures of antiestrogenic drugs and their activities were evaluated by estrogen receptor alpha (ERalpha) binding assay and transactivation assay using human breast cancer cell line, MCF-7 cells. The m-carborane bisphenol 5 exhibited about a thousand times more potent ER agonistic activity than the o-carborane bisphenol 11. The m-carborane bisphenol structure appears to be a favorable hydrophobic pharmacophore for the development of novel selective estrogen receptor modulators (SERMs).
基于抗雌激素药物的结构制备了一系列间碳硼烷衍生物，并通过雌激素受体α（ERα）结合试验和使用人乳腺癌细胞系MCF-7细胞的反式激活试验评估了它们的活性。间碳硼烷双酚5表现出比邻碳硼烷双酚11强约一千倍的ER激动活性。间碳硼烷双酚结构似乎是开发新型选择性雌激素受体调节剂（SERM）的有利疏水药效团。
