Identification and Structure− Activity Relationships of Chromene-Derived Selective Estrogen Receptor Modulators for Treatment of Postmenopausal Symptoms

…, RM Kanojia, F Du, G Jian-Zhong, E Pacia…

文献索引：Jain, Nareshkumar; Xu, Jiayi; Kanojia, Ramesh M.; Du, Fuyong; Guo, Jian-Zhong; Pacia, Emmanuel; Lai, Muh-Tsann; Musto, Amy; Allan, George; Reuman, Michael; Li, Xun; Hahn, DoWon; Cousineau, Martin; Peng, Sean; Ritchie, David; Russell, Ronald; Lundeen, Scott; Sui, Zhihua Journal of Medicinal Chemistry, 2009 , vol. 52, # 23 p. 7544 - 7569

全文：HTML全文

被引用次数: 42

摘要

As part of a program aimed at the development of selective estrogen receptor modulators (SERMs), novel chromene scaffolds, benzopyranobenzoxapanes, were discovered. Many compounds showed binding affinity as low as 1.6− 200 nM, displayed antagonist behaviors in the MCF-7 human breast adenocarcinoma cell line as well in Ishikawa cell line with IC50 values in the range 0.2− 360 nM. On the basis of the side chain substitution, various ...