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Literature DB >> 15482947

Pyrazolo[1,5-a]pyrimidines as estrogen receptor ligands: defining the orientation of a novel heterocyclic core.

Dennis R Compton¹, Kathryn E Carlson, John A Katzenellenbogen.

Abstract

We have examined the pyrazolo[1,5-a]pyrimidine scaffold as a novel core structure for estrogen receptor ligands. Attachment of various substituents has helped to define the orientation of this heterocycle in the ligand-binding pocket as one in which a pendant phenol rather than the hydroxylpyrimidine serves as a mimic of the A-ring of estradiol.

Entities: Chemical Gene

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Year: 2004 PMID： 15482947 DOI： 10.1016/j.bmcl.2004.08.046

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

5 in total

1. A facile, regioselective synthesis of novel 3-(N-phenylcarboxamide)pyrazolo[1,5-a]pyrimidine analogs in the presence of KHSO4 in aqueous media assisted by ultrasound and their antibacterial activities.

Authors: Shunan Kaping; Ivee Boiss; Laishram Indira Singha; Philippe Helissey; Jai N Vishwakarma
Journal: Mol Divers Date: 2015-10-28 Impact factor: 2.943

2. A facile environment-friendly one-pot two-step regioselective synthetic strategy for 3,7-diarylpyrazolo[1,5-a]pyrimidines related to zaleplon and 3,6-diarylpyrazolo[1,5-a]pyrimidine-7-amines assisted by KHSO₄ in aqueous media.

Authors: Asem Satyapati Devi; Shunan Kaping; Jai Narain Vishwakarma
Journal: Mol Divers Date: 2015-05-28 Impact factor: 2.943

Pyrazolo[1,5-a]pyrimidines as estrogen receptor ligands: defining the orientation of a novel heterocyclic core.

1. A facile, regioselective synthesis of novel 3-(N-phenylcarboxamide)pyrazolo[1,5-a]pyrimidine analogs in the presence of KHSO4 in aqueous media assisted by ultrasound and their antibacterial activities.

2. A facile environment-friendly one-pot two-step regioselective synthetic strategy for 3,7-diarylpyrazolo[1,5-a]pyrimidines related to zaleplon and 3,6-diarylpyrazolo[1,5-a]pyrimidine-7-amines assisted by KHSO₄ in aqueous media.

3. Phenethyl pyridines with non-polar internal substituents as selective ligands for estrogen receptor beta.

4. Synthesis of novel nitro-substituted triaryl pyrazole derivatives as potential estrogen receptor ligands.

5. 3-(2,4-Dichloro-phen-yl)-5-(4-fluoro-phen-yl)-2-phenyl-7-(trifluoro-meth-yl)pyrazolo-[1,5-a]pyrimidine.