Synthesis and biological activities of some new dibenzopyranones and dibenzopyrans: search for potential oestrogen receptor agonists and antagonists

Some new tricyclic molecules namely substituted dibenzopyranones and dibenzopyrans bridged between the active molecules of 3,4-diaryl chroman and 2,3-diaryl benzopyrans have been synthesised and screened for their oestrogen receptor agonist and antagonist activities. Continuing our search for newer...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2004-05, Vol.12 (9), p.2239-2249
Main Authors: Pandey, Jaya, Jha, Ashok K, Hajela, K
Format: Article
Language:English
Subjects:
Agonists
Animals
Antagonists
Biological and medical sciences
Bone Resorption
Dibenzopyranones
Dibenzopyrans
Hormones. Endocrine system
Magnetic Resonance Spectroscopy
Medical sciences
Oestrogen receptor
Pharmacology. Drug treatments
Pyrans - chemical synthesis
Pyrans - chemistry
Pyrans - pharmacology
Rats
Rats, Sprague-Dawley
Receptors, Estrogen - agonists
Receptors, Estrogen - antagonists & inhibitors
Receptors, Estrogen - metabolism
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Summary:Some new tricyclic molecules namely substituted dibenzopyranones and dibenzopyrans bridged between the active molecules of 3,4-diaryl chroman and 2,3-diaryl benzopyrans have been synthesised and screened for their oestrogen receptor agonist and antagonist activities. Continuing our search for newer oestrogen agonists or antagonists and extending our work on the exploration of benzopyran related compounds, some new tricyclic molecules bridged between the active molecules of 3,4-diaryl chroman and 2,3-diaryl benzopyrans have been synthesised. Structural modifications at different positions with elements known to impart agonist or antagonist activities have been carried out to prepare the desired molecules. The target compounds were screened for their anti-osteoporotic (agonist) and anti-uterotrophic (antagonist) activities and were found to be moderately active.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2004.02.018