75950-52-6Relevant articles and documents
Activity-guided isolation of an antiandrogenic compound of Pygeum africanum
Schleich, Sonja,Papaioannou, Maria,Baniahmad, Aria,Matusch, Rudolf
, p. 547 - 551 (2007/10/03)
Inactivation of the androgen receptor (AR) through androgen ablation and treatment with antiandrogens is a major goal in the therapy for prostate hyperplasia and prostate cancer. Bioactivity-directed fractionation of a selective dichloromethane extract from the stem bark of Pygeum africanum led to the isolation of the antiandrogenic compound atraric acid. Its activity was examined by an androgen receptor responsive reporter gene assay. For lead structure optimization we transformed the natural occurring compound atraric acid into its ethyl, n-propyl and n-butyl esters and their antiandrogenic activities were examined as well. In addition, benzoic acid was isolated. The structures of all compounds were determined and characterized by means of 1H- and 13C-NMR, HR-EI-mass, IR and UV spectroscopy. Georg Thieme Verlag KG Stuttgart.
Convenient Syntheses of Alkyl β-Resorcylate Derivatives
Barrett, Anthony G. M.,Morris, Timothy M.,Barton, Derek H. R.
, p. 2272 - 2277 (2007/10/02)
Syntheses of methyl 2,4-dihydroxy-6-methyl- (1a) and -3,6-dimethylbenzoates (1b) and methyl 2,4-dihydroxy-6-pentylbenzoate (1c) are described.Condensation reactions of dimethyl sodiomalonate with the dianion derived from pentane-2,4-dione or the dimerisation of the methyl acetoacetate dianion or the acetylation of the trianion derived from methyl 3,5,7-trioxo-octanoate gave (1a) (78percent) after work-up at pH 9.Analogous convenient, short, optimised syntheses of (1b and c) are given in detail.