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Bioorg Chem ; 113: 105017, 2021 08.
Artículo en Inglés | MEDLINE | ID: mdl-34091288

RESUMEN

Breast cancer, emerging malignancy is common among women due to overexpression of estrogen. Estrogens are biosynthesized from androgens by aromatase, a cytochrome P450 enzyme complex, and play a pivotal role in stimulating cell proliferation. Therefore, deprivation of estrogen by blocking aromatase is considered as the effective way for the inhibition and treatment of breast cancer. In recent years, various non-steroidal heterocyclic functionalities have been extensively developed and studied for their aromatase inhibition activity. This review provides information about the structural-activity relationship of heterocycles (Type II) towards aromatase. This aids the medicinal chemist around the significance of different heterocyclic moieties and helps to design potent aromatase inhibitors.


Asunto(s)
Inhibidores de la Aromatasa/química , Aromatasa/metabolismo , Compuestos Heterocíclicos/química , Aromatasa/química , Inhibidores de la Aromatasa/metabolismo , Inhibidores de la Aromatasa/uso terapéutico , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/patología , Diseño de Fármacos , Estrógenos/metabolismo , Femenino , Compuestos Heterocíclicos/metabolismo , Compuestos Heterocíclicos/uso terapéutico , Humanos , Relación Estructura-Actividad
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