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Insights into the Synthesis of Steroidal A-Ring Olefins
Varela, Carla M.; Roleira, Fernanda M. F.; Costa, Saul C. P.; Tinto, Alexandra S. C. T.; Martins, Ana I. O. S.; Carvalho, Rui A.; Teixeira, Natércia A.one (5), from the D1-3-keto enone, (5a,17b)-3-oxo-5-androst-1-en-17-yl acetate (1), through a strategy involving the reaction of D1-3-hydroxy allylic alcohol, 3b-hydroxy-5a-androst-1-en-17b-yl acetate (2), with SOCl2 , was revisited in order to prepare and biologically evaluate 5 as aromatase inhibitor for breast cancer treatment. Surprisingly, the followed strategy also afforded the isomeric D2-olefin 6 as a b...
New steroidal 17b-carboxy derivatives present anti-5a-reductase activity and an...
Amaral, Cristina; Varela, Carla; Correia-da-Silva, Georgina; da Silva, Elisário Tavares; Carvalho, R. A.; Costa, Saul C. P.; Cunha, Sara C.The androgens testosterone (T) and dihydrotestosterone (DHT), besides playing an important role in prostate development and growth, are also responsible for the development and progression of benign prostate hyperplasia (BPH) and prostate cancer. Therefore, the actions of these hormones can be antagonized by preventing the irreversible conversion of T into DHT by inhibiting 5a-reductase (5a-R). This has been a ...
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 ...
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