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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 in vivo 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.
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