554430-78-3Relevant academic research and scientific papers
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha
Zhang, Birong,Kiefer, James R.,Blake, Robert A.,Chang, Jae H.,Hartman, Steven,Ingalla, Ellen Rei,Kleinheinz, Tracy,Mody, Vidhi,Nannini, Michelle,Ortwine, Daniel F.,Ran, Yingqing,Sambrone, Amy,Sampath, Deepak,Vinogradova, Maia,Zhong, Yu,Nwachukwu, Jerome C.,Nettles, Kendall W.,Lai, Tommy,Liao, Jiangpeng,Zheng, Xiaoping,Chen, Hai,Wang, Xiaojing,Liang, Jun
, p. 905 - 911 (2019)
Despite tremendous progress made in the understanding of the ERα signaling pathway and the approval of many therapeutic agents, ER+ breast cancer continues to be a leading cause of cancer death in women. We set out to discover compounds with a dual mechan
FUSED TETRACYCLIC HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
-
, (2015/07/07)
The present invention relates to novel Fused Tetracyclic Heterocyclic Compounds of Formula I: (I), wherein A, A', R2A, R2B, R7, R8, R9, and R10 are defined herein. The compounds and their p
FUSED TETRACYCLIC HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
-
, (2015/07/07)
The present invention relates to novel Fused Tetracyclic Heterocyclic Compounds of Formula (I): wherein A, A', R2A, R2B, R7, R8, R9 and R10 are defined herein. The compounds and their pharm
Identification and structure - Activity relationships of chromene-derived selective estrogen receptor modulators for treatment of postmenopausal symptoms
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
scheme or table, p. 7544 - 7569 (2010/06/13)
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 behavior
Synthesis of tetracyclic heterocompounds as selective estrogen receptor modulators. Part 1. Process development for scale-up of 2,5,8-substituted 5,11 -dihydrochromeno[4,3-c]chromene derivatives
Li, Xun,Reuman, Michael,Russell, Ronald K.,Adams, Richard,Ma, Robert,Beish, Sandra,Branum, Shawn,Youells, Scott,Roberts, Jerry,Jain, Nareshkumar,Kanojia, Ramesh,Sui, Zhihua
, p. 414 - 421 (2012/12/31)
Unsymmetrical benzopyranobenzopyran compounds are novel selective estrogen receptor modulators (SERMs). A reproducible and nonchromatographic process was developed to prepare multihundred gram quantities of 5-(4-(2-(piperidin-1-yl) ethoxy)-phenyl)-5,11-di
Development of a scalable synthetic process for selective bromination of 4-methyl-3,7-substituted coumarins
Li, Xun,Jain, Nareshkumar,Russell, Ronald K.,Ma, Robert,Branum, Shawn,Xu, Jiayi,Sui, Zhihua
, p. 354 - 360 (2012/12/22)
The hydroxyl-protected coumarin derivatives 6a-e of 4-methyl-3-(2,4- dihydroxyphenyl)-7-hydroxycoumarin (4) are key intermediates in the synthesis of unsymmetrical benzopyranobenzopyran compounds, a novel series of selective estrogen receptor modulators (
A facile synthesis of an unsymmetric benzopyranobenzopyran ring system
Kanojia, Ramesh M.,Jain, Nareshkumar,Xu, Jiayi,Sui, Zhihua
, p. 5837 - 5839 (2007/10/03)
A facile route to the synthesis of an unsymmetric benzopyranobenzopyran ring system is described. A key feature of this synthesis incorporates a tandem deprotection-cyclization strategy to construct the C-ring of the tetracyclic system.
