448956-60-3Relevant articles and documents
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids
Link,Sorensen, Bryan K.,Lai, Chunqiu,Wang, Jiahong,Fung, Steven,Deng, Daisy,Emery, Maurice,Carroll, Sherry,Grynfarb, Marlena,Goos-Nilsson, Annika,Von Geldern, Thomas
, p. 4173 - 4178 (2004)
The synthesis, activity, metabolic stability, and pharmacokinetics of steroidal and nonsteroidal glucocorticoid receptor modulator-statin hybrids is reported. Potent steroidal antagonist-statin hybrids like 22 (h-GR binding IC50=7nM) and nonsteroidal modulator hybrids like 16 (h-GR binding IC50=2nM) were discovered. Appending a 'statin'-like diol-acid group to the modulators dramatically improved metabolic stability (and in some cases hepatocyte activity), but did not impart hepatoselectivity.
GLUCOCORTICOID RECEPTOR MODULATORS
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, (2008/06/13)
Compounds of formula (I) or pharmaceutically acceptable salts thereof are novel glucocorticoid receptor modulators and are useful for treating type II diabetes in a mammal.