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- W2947589481 endingPage "708" @default.
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- W2947589481 abstract "Aromatase is a rate-limiting enzyme for estrogen biosynthesis that is overproduced in breast cancer tissue. To block the growth of breast tumors, aromatase inhibitors (AIs) are employed to bind and inhibit aromatase in order to lower the amount of estrogen produced in the body. Although a number of synthetic aromatase inhibitors have been released for clinical use in the treatment of hormone-receptor positive breast cancer, these inhibitors may lead to undesirable side effects (e.g. increased rash, diarrhea and vomiting; effects on the bone, brain and heart) and therefore, the search for novel AIs continues. Over the past decades, there has been an intense effort in employing medicinal chemistry and quantitative structure-activity relationship (QSAR) to shed light on the mechanistic basis of aromatase inhibition. To the best of our knowledge, this article constitutes the first comprehensive review of all QSAR studies of both steroidal and non-steroidal AIs that have been published in the field. Herein, we summarize the experimental setup of these studies as well as summarizing the key features that are pertinent for robust aromatase inhibition." @default.
- W2947589481 created "2019-06-07" @default.
- W2947589481 creator A5043577834 @default.
- W2947589481 creator A5069155677 @default.
- W2947589481 creator A5084444175 @default.
- W2947589481 date "2018-01-01" @default.
- W2947589481 modified "2023-09-29" @default.
- W2947589481 title "Towards understanding aromatase inhibitory activity via QSAR modeling." @default.
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- W2947589481 doi "https://doi.org/10.17179/excli2018-1417" @default.
- W2947589481 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6123608" @default.
- W2947589481 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30190660" @default.
- W2947589481 hasPublicationYear "2018" @default.
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