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Synthesis and biochemical studies of 17-substituted androst-3-enes and 3,4-epox...

Cepa, Margarida M. D. S.; Silva, Elisiário J. Tavares da; Correia-da-Silva, Georgina; Roleira, Fernanda M. F.; Teixeira, Natércia A. A.

http://www.sciencedirect.com/science/article/B6TC9-4T0WJXG-2/2/58305e64e3c068f352293a693f168db2


Structure−Activity Relationships of New A,D-Ring Modified Steroids as Aromatase...

Cepa, Margarida M. D. S.; Silva, Elisiário J. Tavares da; Correia-da-Silva, Georgina; Roleira, Fernanda M. F.; Teixeira, Natércia A. A.

Inhibition of aromatase is an efficient approach for the prevention and treatment of breast cancer. New A,D-ring modified steroid analogues of formestane and testolactone were designed and synthesized and their biochemical activity was investigated in vitro in an attempt to find new aromatase inhibitors and to gain insight into their structure−activity relationships (SAR). All compounds tested were less active ...


Improved syntheses of aromatase inhibitors and neuroactive steroids efficient o...

Neves, André S. Campos; Melo, Maria Luisa Sá e; Moreno, Maria José S. M.; Silva, Elisiário J. Tavares da; Salvador, Jorge A. R.; Costa, Saul P. da

An Henbest reduction, followed by the preparation of a silyl enol ether and oxidation in situ with m-CPBA has led to the neurosteroids 3[alpha]-hydroxy- and 3[alpha],21-dihydroxy-5[alpha]-pregnanolones. Using testosterone as starting material, a new short synthesis of an aromatase inhibitor, 4-OHA, has been achieved through hydroboration/oxidation followed by a Swern type oxidation and epimerization. Another ar...


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