Synthesis and pharmacological evaluation of novel cis-3,4-diaryl-hydroxychromanes as high affinity partial agonists for the estrogen receptor

被引：33

作者：

Bury, PS ^{[1
]}

Christiansen, LB ^{[1
]}

Jacobsen, P ^{[1
]}

Jorgensen, AS ^{[1
]}

Kanstrup, A ^{[1
]}

Nærum, L ^{[1
]}

Bain, S ^{[1
]}

Fledelius, C ^{[1
]}

Gissel, B ^{[1
]}

Hansen, BS ^{[1
]}

Korsgaard, N ^{[1
]}

Thorpe, SM ^{[1
]}

Wassermann, K ^{[1
]}

机构：

[1] Novo Nordisk AS, DK-2760 Malov, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 01期

关键词：

D O I：

10.1016/S0968-0896(01)00257-7

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The syntheses and in vitro pharmacological evaluation of a number of cis-3,4-diaryl-hydroxy-chromanes are reported, along with the results of a thorough in vivo profiling of the tissue-selective estrogen partial-agonist NNC 45-0781 [3, (-)-(3S,4R)-7-hydroxy-3-phenyl-4-(4-(2-pyrrolidinoethoxy)phenyl)chromane]. These studies showed that NNC 45-0781 is a very promising candidate for the prevention of post-menopausal osteoporosis, and the treatment of other health issues related to the loss of endogenous estrogen production. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：125 / 145

页数：21

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