Misawa Takashi, Tanaka Katsuya, Demizu Yosuke, Kurihara Masaaki
National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo, Japan.
National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo, Japan.
Bioorg Med Chem Lett. 2017 Jun 1;27(11):2590-2593. doi: 10.1016/j.bmcl.2017.03.066. Epub 2017 Mar 24.
Steroids are important components of cell membranes and are involved in several physiological functions. A diphenylmethane (DPM) skeleton has recently been suggested to act as a mimetic of the steroid skeleton. However, difficulties are associated with efficiently introducing different substituents between two phenyl rings of the DPM skeleton, and, thus, further structural development based on the DPM skeleton has been limited. We herein developed an efficient synthetic method for introducing different substituents into two phenyl rings of the DPM skeleton. We also synthesized DPM-based estrogen receptor (ER) modulators using our synthetic method and evaluated their ER transcriptional activities.
类固醇是细胞膜的重要组成部分，并参与多种生理功能。最近有人提出二苯甲烷（DPM）骨架可作为类固醇骨架的模拟物。然而，在DPM骨架的两个苯环之间有效引入不同取代基存在困难，因此，基于DPM骨架的进一步结构开发受到限制。我们在此开发了一种将不同取代基引入DPM骨架两个苯环的有效合成方法。我们还使用我们的合成方法合成了基于DPM的雌激素受体（ER）调节剂，并评估了它们的ER转录活性。
