对称的4,4'-（哌啶-4-基亚甲基）双酚衍生物作为新型可调雌激素受体（ER）调节剂。
Symmetric 4,4'-(piperidin-4-ylidenemethylene)bisphenol derivatives as novel tunable estrogen receptor (ER) modulators.
作者信息
Sato Manabu, Ohta Kiminori, Kaise Asako, Aoto Sayaka, Endo Yasuyuki
机构信息
Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai 981-8558, Japan.
Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai 981-8558, Japan.
出版信息
Bioorg Med Chem. 2016 Mar 1;24(5):1089-94. doi: 10.1016/j.bmc.2016.01.035. Epub 2016 Jan 18.
We designed and synthesized 4,4'-(piperidin-4-ylidenemethylene)bisphenol derivatives as novel tunable estrogen receptor (ER) modulators. The introduction of hydrophobic substituents on the nitrogen atom of the piperidine ring enhanced ERα binding affinity. In addition, the introduction of four methyl groups adjacent to the piperidine ring nitrogen atom remarkably enhanced ERα binding affinity. N-Acetyl-2,2,6,6-tetramethylpiperidine derivative 3b showed high ERα binding affinity, high MCF-7 cell proliferation inducing activity, and high metabolic stability in rat liver S9 fractions.
我们设计并合成了4,4'-(哌啶-4-基亚甲基)双酚衍生物作为新型的可调节雌激素受体(ER)调节剂。在哌啶环的氮原子上引入疏水取代基增强了ERα结合亲和力。此外，在哌啶环氮原子相邻位置引入四个甲基显著增强了ERα结合亲和力。N-乙酰基-2,2,6,6-四甲基哌啶衍生物3b在大鼠肝脏S9组分中表现出高ERα结合亲和力、高MCF-7细胞增殖诱导活性和高代谢稳定性。
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