Synthesis, antiproliferative evaluation and in silico studies of a novel steroidal spiro morpholinone

Cobos-Ontiveros, Luis A; Romero-Hernández, Laura L.; Mastranzo-Sánchez, Eduardo B; Colín-Lozano, Blanca; Puerta, Adrián; Padrón, José M.; Merino-Montiel, Penélope; Báez, José Luis Vega; Montiel‐Smith, Sara

doi:10.1016/j.steroids.2023.109173

Cited by 1 publication

(2 citation statements)

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“…Abiraterone (GI 50 values in the range of 24–100 μM) and galeterone (GI 50 values in the range of 2.1–10 μM) were used as reference drugs. To explain the mechanism of action of the compounds, molecular docking tests were performed, which demonstrated the ability of active molecules to inhibit aromatase [ 13 ].…”

Section: Aromatase Inhibitorsmentioning

confidence: 99%

“…Abiraterone (GI50 values in the range of 24-100 µM) and galeterone (GI50 values in the range of 2.1-10 µM) were used as reference drugs. To explain the mechanism of action of the compounds, molecular docking tests were performed, which demonstrated the ability of active molecules to inhibit aromatase [13]. In 2023, Roleira et al carried out work as a result of which a series of steroid molecules that were potential aromatase inhibitors were designed, synthesized, and tested for biological activity.…”

Section: Steroidal Aromatase Inhibitorsmentioning

confidence: 99%

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Aromatase Inhibitors as a Promising Direction for the Search for New Anticancer Drugs

Janowska,

Holota,

Lesyk

et al. 2024

Molecules

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Aromatase is an enzyme that plays a crucial role in the biosynthesis of estrogens, which are hormones that contribute to the growth of certain types of breast cancer. In particular, aromatase catalyzes the conversion of androgens (male hormones) into estrogens (female hormones) in various tissues, including the adrenal glands, ovaries, and adipose tissue. Given the role of estrogen in promoting the growth of hormone-receptor-positive breast cancers, aromatase has become an important molecular target for the development of anticancer agents. Aromatase inhibitors can be classified into two main groups based on their chemical structure: steroidal and non-steroidal inhibitors. This work presents a review of the literature from the last ten years regarding the search for new aromatase inhibitors. We present the directions of search, taking into account the impact of structure modifications on anticancer activity.

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Section: Aromatase Inhibitorsmentioning

confidence: 99%

Section: Steroidal Aromatase Inhibitorsmentioning

confidence: 99%