Reference

Structure-Guided Optimization of Estrogen Receptor Binding Affinity and Antagonist Potency of Pyrazolopyrimidines with Basic Side Chains

All Rights Reserved. Structure-Guided Optimization of Estrogen Receptor Binding Affinity and Antagonist Potency of Pyrazolopyrimidines with Basic Side Chains. Zhou, Hai-Bing; Sheng, Shubin; Compton, Dennis R.; Kim, Younchang; Joachimiak, Andrzej; Sharma, Sanjay; Carlson, Kathryn E.; Katzenellenbogen, Benita S.; Nettles, Kendall W.; Greene, Geoffrey L.; Katzenellenbogen, John A. (Department of Chemistry, University of Illinois, Urbana, IL 61801, USA). Journal of Medicinal Chemistry, 50(2), 399-403 (English) 2007 American Chemical Society. CODEN: JMCMAR. ISSN: 0022-2623. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) 2,3-Diarylpyrazolo[1,5-a]pyrimidines are estrogen receptor (ER) antagonists of modest potency that we have described previously. Guided by the crystal structure of an ER-ligand complex that we have obtained with one of these compds.In this experiment, several chemicals are used like 924907-80-2 , we prepd. analogs that contain a basic side chain at the 2- or 3-aryl group and quickly found one that, according to the structure-based prediction, shows an increase in binding affinity and antagonist potency and a loss of residual agonist activity. .

A convenient synthesis of trans- and cis-3,4',5-trihydroxystilbene

All Rights Reserved. Several substances are used for example 104-47-2 and 61434-67-1 which are their cas registry numbers. A convenient synthesis of trans- and cis-3,4',5-trihydroxystilbene. Wang, Zhi-xin; Zhang, Xue-jing; Zhou, Yue; Zou, Yong (Guangzhou Institute of Chemistry, Chinese Academy of Sciences, Guangzhou 510650, Peop. Rep. China). Journal of Chinese Pharmaceutical Sciences, 14(4), 204-208 (Chinese) 2005 Journal of Chinese Pharmaceutical Sciences. CODEN: JCHSE4. ISSN: 1003-1057. DOCUMENT TYPE: Journal CA Section: 26 (Biomolecules and Their Synthetic Analogs) Title compd. was prepd. from 3,5-dimethoxybenzaldehyde and 4-methoxyphenylacetonitrile via condensation reaction to form stilbene skeleton, after hydrolysis, decarboxylation, and demethylation to obtained trans-3,4',5-trihydroxystilbene (Resveratrol), which can be converted to its cis-isomer by photochem. isomerization. A facile method for the synthesis of trans- and cis-hydroxystilbenes from readily available starting materials was established. .