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Molecules, Vol. 28, Pages 789: An Exemestane Derivative, Oxymestane-D1, as a New Multi-Target Steroidal Aromatase Inhibitor for Estrogen Receptor-Positive (ER+) Breast Cancer: Effects on Sensitive and Resistant Cell Lines
M. F. Roleira Around 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 drugs are emerging, as they present higher efficacy and lower toxicity in comparison to standard options. Considering this, this work aimed to investigate the anti-cancer properties an...
Source: Molecules - January 12, 2023 Category: Chemistry Authors: Cristina Amaral Georgina Correia-da-Silva Cristina Ferreira Almeida Maria Jo ão Valente Carla Varela Elisi ário Tavares-da-Silva Anne Marie Vinggaard Nat ércia Teixeira Fernanda M. F. Roleira Tags: Article Source Type: research

Molecules, Vol. 26, Pages 1488: Development of CDK4/6 Inhibitors: A Five Years Update
tacuzzi The inhibition of cyclin dependent kinases 4 and 6 plays a role in aromatase inhibitor resistant metastatic breast cancer. Three dual CDK4/6 inhibitors have been approved for the breast cancer treatment that, in combination with the endocrine therapy, dramatically improved the survival outcomes both in first and later line settings. The developments of the last five years in the search for new selective CDK4/6 inhibitors with increased selectivity, treatment efficacy, and reduced adverse effects are reviewed, considering the small-molecule inhibitors and proteolysis-targeting chimeras (PROTACs) approaches, main...
Source: Molecules - March 9, 2021 Category: Chemistry Authors: Alessandra Ammazzalorso Mariangela Agamennone Barbara De Filippis Marialuigia Fantacuzzi Tags: Review Source Type: research