New steroidal aromatase inhibitors: biological effects in hormone-dependent breast cancer cell models

• Autor(a) principal: Sobral, Ana Filipa
• Data de Publicação: 2016
• Outros Autores: Amaral, Cristina, Varela, Carla, Tavares, Elisiário, Roleira, Fernanda, Correia-Da-Silva, Georgina, Teixeira, Natércia, Campos, Saul
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
• Texto Completo: https://doi.org/10.34624/captar.v6i1.13117

Aromatase inhibitors (AIs) are currently used as a first-line therapeutic approach for hormone-dependent (ER+) breast tumors in postmenopausal women, the most common type of cancer diagnosed among women, in which estrogen plays a key role. Aromatase is the enzyme responsible for estrogen biosynthesis, so its inhibition results in estrogen suppression, avoiding tumor growth. However, the existence of side-effects with the current AIs used in clinic, such as development of therapy resistance and bone loss, justifies the search for new AIs. In the past few years, several steroidal compounds have been synthesized with structural modifications in androstenedione, the aromatase substrate, in order to achieve maximum inhibitory effects on aromatase. The present work aims to continue this research line, so newly synthesized steroidal compounds (49, 50, 51 and 52) with structural modifications on A-, B- and D-rings are under biological evaluation, using different human breast cancer cell lines, an ER+ aromatase overexpressing breast cancer cell line (MCF-7aro), an ER- breast cancer cell line (SK-BR-3) and a late stage of acquired endocrine resistance cell line (LTEDaro). [...]