Arányi P, Náray A, Ninh N V, Fekete G, Tóth J, Horváth I
Steroids. 1983 Oct;42(4):409-15. doi: 10.1016/0039-128x(83)90139-3.
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.
对新型合成糖皮质激素类似物进行了受体结合和糖皮质激素活性测试。它们具有不寻常的结构，因为它们具有3-氯而非3-氧代官能团。氟化糖皮质激素的3-氯类似物与大鼠肝脏糖皮质激素受体形成极其稳定的复合物。氟轻松醋酸酯的3-氯衍生物也具有体内糖皮质激素活性。它能非常有效地诱导肝脏中的酪氨酸转氨酶并抑制胸腺中的胸苷激酶。得出的结论是，3-氯类似物可能保留糖皮质激素活性以及与糖皮质激素受体蛋白结合的能力。
