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Diaryl-dialkyl-substituted pyrazoles: regioselective synthesis and binding affinity for the estrogen receptor.

Abstract：

:We have developed two novel series of tetrasubstituted pyrazoles, embodying 1,3-diaryl-4,5-dialkyl or 3,5-diaryl-1,4-dialkyl substitution patterns. The scope of a regioselective method, developed by us earlier, was expanded to allow the synthesis of the first series of these tetrasubstituted pyrazoles directly from alpha,beta-unsaturated ketones. The binding affinity of some of these pyrazoles for the estrogen receptor (ER) subtypes ERalpha and ERbeta is very high, and the overall affinity pattern suggests the importance of three phenol substituents for high affinity, ERalpha-selective binding.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Nishiguchi GA,Rodriguez AL,Katzenellenbogen JA

doi

10.1016/s0960-894x(02)00057-4

subject

Has Abstract

pub_date

2002-03-25 00:00:00

pages

947-50

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960894X02000574

journal_volume

12

pub_type

杂志文章

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