Synthesis and evaluation of hexahydrochrysene and tetrahydrobenzofluorene ligands for the estrogen receptor

Synthesis and evaluation of hexahydrochrysene and tetrahydrobenzofluorene ligands for the estrogen receptor
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DOI:
10.1016/s0960-894x(01)00189-5
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发表时间:
2001-05-21
影响因子:
2.7
通讯作者:
Katzenellenbogen, JA
Katzenellenbogen, JA
中科院分区:
医学4区
文献类型:
--
作者:
Tedesco, R;Youngman, MK;Katzenellenbogen, JA

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为了制备新的雌激素受体(ER)配体,我们开发了一种简单的方法来取代六氢芘和四氢苯并[a]芴体系。在这些系统中加入取代基,包括碱性侧链,并对其与ER α和ER β的结合亲和力进行了评估,并在某些情况下对其转录活性进行了评估。2001爱思唯尔科学有限公司版权所有。
To prepare novel estrogen receptor (ER) ligands, we have developed a facile approach to substituted hexahydrochrysene and tetrahydrobenzo[a]fluorene systems. Substituents, including basic side chains, were added to these systems, and their binding affinity to ER alpha and ER beta, and in some cases their transcriptional activity were evaluated. (C) 2001 Elsevier Science Ltd. All rights reserved.