2 documents found, page 1 of 1
An Exemestane Derivative, Oxymestane-D1, as a New Multi-Target Steroidal Aromat...
Amaral, Cristina; Correia-da-Silva, Georgina; Almeida, Cristina Ferreira; Valente, Maria João; Varela, Carla; Tavares-da-Silva, ElisiarioAround 70-85% of all breast cancer (BC) cases are estrogen receptor-positive (ER+). The third generation of aromatase inhibitors (AIs) is the first-line treatment option for these tumors. Despite their therapeutic success, they induce several side effects and resistance, which limits their efficacy. Thus, it is crucial to search for novel, safe and more effective anti-cancer molecules. Currently, multi-target d...
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...