3-chloro-1, 3, 5-pregnatriene derivatives with glucocorticoid activity |
| |
Authors: | P. Arányi A. Náray N. Vi Ninh Gy. Fekete J. Tóth I. Horváth |
| |
Affiliation: | 1. Second Institute of Biochemistry, Semmelweis University Medical School, H-1444 Budapest, Hungary;2. Chemical Works of Gedeon Richter Ltd., Budapest, Hungary |
| |
Abstract: | Novel synthetic glucocorticoid analogues were tested for receptor binding and glucocorticoid activity. They were of unusual structure, insofar as they had a 3-chloro rather than a 3-oxo function. 3-Chloro analogues of fluorinated glucocorticoids formed extremely stable complexes with the rat liver glucocorticoid receptor. 3-Chloro derivative of fluocinolone acetonide also had glucocorticoid activity. It induced tyrosine aminotransferase in the liver and repressed thymidine kinase in the thymus very effectively. It is concluded that 3-chloro analogues may retain glucocorticoid activity as well as the ability to bind to the glucocorticoid receptor protein. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|