CYCLIC 16α,17α-Ketals AND ACETALS OF 9α-Fluoro-16α-Hydroxy-Cortisol AND -PREDNISOLONE

Heterogeneity of Binding Sites for Glucocorticoid and the Glucocorticoid-Receptor Complex in Rat Livers

“…The glucocorticoid-receptor complex binding to the nuclear fraction was temperature-dependent, saturable, small in amount and of high affinity. The affinity and number of the glucocorticoid-receptor complex binding to the nuclear fraction were altered according to the glucocorticoid.Both the Bmax of nuclear gluco corticoid-receptor complex binding and the affinity of glucocorticoid to the cyto plasmic fraction were correlated with the relative anti-inflammatory potencies of glucocorticoids reported by Hynes and Murad (1980) and Fried et al (1958). These results suggest that the number of nuclear binding sites of the glucocorticoid receptor complex depends on the ligand steroid which is bound to the receptor of the cytoplasmic fraction and may be involved in physiological and pharmacological potencies of the glucocorticoid in addition to the affinity of the glucocorticoid to the receptor.…”

A Concise Synthesis of Enantioenriched Fluorinated Carbocycles

“…Since the discovery by Fried et al [1] that fluorocortisone is much more potent than the nonfluorinated parent compound, the incorporation of fluorine in drug design has been a powerful strategy to improve properties such as bioavailability and lipophilicity. [2] In addition, with the role of chirality firmly established in medicinal chemistry, efficient methods for the selective formation of fluorinated stereogenic centers are in increasing demand.…”

In-VITRO SYNTHESIS OF ANDROGEN FROM PREGNENOLONE IN THE TESTES OF THE GOAT (CAPRA HIRCUS) AND IDENTIFICATION OF 5-Pregnene-3β,17α,20α-Triol AS AN INTERMEDIATE IN THE METABOLIC PATHWAY OF PREGNENOLONE

“…The product showed identical mobilities to those of 17a,20a-dihydroxy-4-pregnen-3-one on the thin-layer chromatograms developed with various solvent systems. The reaction product of metabolite X with acetone in concentrated HC1 was less polar than the original mobility on the thin-layer chromatogram, indicating that acetonide was formed in the molecule (Fried, Borman, Kessler, Grabowich & Sabo, 1958). Furthermore, the diacetate of metabolite X formed with acetic anhydride and pyridine (1:1, v/v) at room temperature was further acetylated with 0-8% /^-toluene sulphonic acid in acetic acid and acetic anhydride (5:1, v/v) with reflux (Turner, 1953).…”