Richardson Timothy I, Norman Bryan H, Lugar Charles W, Jones Scott A, Wang Yong, Durbin Jim D, Krishnan Venkatesh, Dodge Jeffrey A
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
Bioorg Med Chem Lett. 2007 Jul 1;17(13):3570-4. doi: 10.1016/j.bmcl.2007.04.051. Epub 2007 Apr 25.
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here we describe structure-activity relationship studies that led to the discovery of bezopyran 5b. X-ray crystal structures of 5b and a non-selective analog 5c in ERalpha help explain the observed selectivity of the benzopyran platform.
苯并吡喃是选择性雌激素受体（ER）β激动剂（SERBAs），它们以相反的方向与ER亚型α和β结合。在此，我们描述了导致发现苯并吡喃5b的构效关系研究。5b和一种非选择性类似物5c在ERα中的X射线晶体结构有助于解释观察到的苯并吡喃平台的选择性。
