Estrogen designer

Ariyo AA, Villablanca AC. Estrogens and lipids. Can HRT designer estrogens, and phytoestrogens reduce cardiovascular risk markers after menopause Postgrad Med 2002 lll(l) 23-30. 

Miscellaneous Pharmaceutical Processes. Solvent extraction is used for the preparation of many products that ate either isolated from naturally occurring materials or purified during synthesis. Among these are sulfa dmgs, methaqualone [72-44-6] phenobarbital [50-06-6] antihistamines, cortisone [53-06-5] estrogens and other hormones (qv), and reserpine [50-55-5] and alkaloids (qv). Common solvents for these appHcations are chloroform, isoamyl alcohol, diethyl ether, and methylene chloride. Distribution coefficient data for dmg species are important for the design of solvent extraction procedures. These can be determined with a laboratory continuous extraction system (AKUEVE) (244). 

Finally, a major question in SERM development is whether the new compounds will behave like estrogens with respect to cardiovascular events, which would be a worthless property given the results of the WHI trial (Writing Group for the Women s Health Initiative Investigators 2002 Women s Health Initiative Steering Committee 2004). This is a complex issue that will depend on the unique profile of action of the new SERM on the different components of the atherosclerosis process and the patient population and study design and conduct that is implemented. 

Miller CP, Collini MD, Tran BD, Harris HA, Kharode YP, Marzolf JT, et al. (2001) Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. J MedChem 44 1654-1657... 

I. El labri, S. De Lauzon, and N. Cittanova, Estrogen fluoroimmunoassay with a fluorimeter designed for low-intensity light detection, Anal. Chim. Acta 227, 129-134(1989)... 

Example 17 Bertozzi and associates in their studies on sulfotransferases have performed synthesis of a bisubstrate analogue designed to inhibit estrogen sulfotransferase [45]. Synthesis of this diphosphate depends on the coupling of two phosphates prepared by phosphoroamidite methodology. The synthesis utilizes differently protected 3 -phosphoadenosine-5 -phos-phate allowing selective functionalization of the 5 -phosphate with the sulfate acceptor mimic. 

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