91667-86-6Relevant articles and documents
Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B
He, Hai-Bing,Gao, Li-Xin,Deng, Qi-Feng,Ma, Wei-Ping,Tang, Chun-Lan,Qiu, Wen-Wei,Tang, Jie,Li, Jing-Ya,Li, Jia,Yang, Fan
, p. 7237 - 7242 (2012)
Protein tyrosine phosphatase 1B (PTP1B) is a major negative regulator of both insulin and leptin signals. For years, inhibiting of PTP1B has been considered to be a potential therapeutics for treating Type 2 diabetes and obesity. Recently, we recognized lithocholic acid (LCA) as a natural inhibitor against PTP1B (IC50 = 12.74 μM) by a vertical screen for the first time. Further SAR research was carried out by synthesizing and evaluating a series of compounds bearing two methyls at C-4 position and a fused heterocycle to ring A. Among them, compound 14b achieved a PTP1B inhibitory activity about eightfold than LCA and a 14-fold selectivity over the homogenous enzyme TCPTP.
SYNTHESE D'ANTIBIOTIQUES TRITERPENIQUES A PARTIR D'ACIDES BILIAIRES. IV . ETUDE DE L'HYDROGENATION CATALYTIQUE DU DIMETHYL-4,4 CHOLENE-5 ONE-3 OATE-24 DE METHYLE.
Aranda, G.,Fetizon, M.,Tayeb, N.
, p. 4147 - 4158 (2007/10/02)
Catalytic hydrogenation of methyl 4,4 dimethyl chol-5 en-3-one-24 oate, prepared from lithocholic acid has been carefully studied in a variety of conditions (solvent, temperature, pressure, nature and amount of catalyst) .Fairly mild conditions have been found, which lead to the 5α dihydroderivative, and do not affect the Δ8(9) double bond of lanosterol.Therefore, one of the major difficulties of the conversion of bile acids into tetracyclic triterpene antibiotics has been overcome .
