雌激素受体配体。第11部分：异苯并二氢吡喃和异硫代苯并二氢吡喃的合成与活性
Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
作者信息
Liu Jian, Birzin Elizabeth T, Chan Wanda, Yang Yi Tien, Pai Lee-Yuh, Dasilva Carolyn, Hayes Edward C, Mosley Ralph T, Dininno Frank, Rohrer Susan P, Schaeffer James M, Hammond Milton L
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2005 Feb 1;15(3):715-8. doi: 10.1016/j.bmcl.2004.11.018.
The ring oxygen and sulfur analogs of lasofoxifene, 1a and 1b, were synthesized in an attempt to impart ERalpha selectivity, as found in the closely related dihydrobenzoxathiin compound I, recently discovered in these laboratories. The resulting isochroman and isothiochroman compounds were found to exhibit equipotent binding affinities to the ER isoforms and were less active in the inhibition of estradiol-triggered uterine growth when compared to I and lasofoxifene.
合成了拉索昔芬的环氧和硫类似物1a和1b，试图赋予其雌激素受体α（ERα）选择性，就像在这些实验室最近发现的密切相关的二氢苯并硫代二氢吡喃化合物I中所发现的那样。结果发现，与化合物I和拉索昔芬相比，所得的异苯并二氢吡喃和异硫代苯并二氢吡喃化合物对ER亚型表现出同等的结合亲和力，并且在抑制雌二醇引发的子宫生长方面活性较低。
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