Pyridine based dual binding site aromatase (CYP19A1) inhibitors

Simons, Claire; Eissa, Ahmed G.; Powell, Lauren E; Gee, Julia Margaret Wendy; Foster, Paul A.

doi:10.1039/d2md00352j

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Aromatase Inhibitors1

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2024

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“…Computational studies of pyridine derivatives identified an alternative access channel lined by Phe221, Gln225, Trp224, and Leu477. This allows further insight into the interactions between non-steroidal aromatase inhibitors and their molecular target [ 48 ].…”

Section: Aromatase Inhibitorsmentioning

confidence: 99%

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%