A review on diverse heterocyclic compounds as the privileged scaffolds in non-steroidal aromatase inhibitors

被引：30

作者：

Rani, Sudesh ^{[1
]}

Raheja, Konpal ^{[1
]}

Luxami, Vijay ^{[1
]}

Paul, Kamaldeep ^{[1
]}

机构：

[1] Thapar Inst Engn & Technol, Sch Chem & Biochem, Patiala 147001, Punjab, India

来源：

BIOORGANIC CHEMISTRY | 2021年 / 113卷

关键词：

Non-steroidal aromatase; Structure-activity relationship; Breast cancer; Heterocycles; Medicinal chemistry; BREAST-CANCER; MOLECULAR DOCKING; BIOLOGICAL CHARACTERIZATION; SELECTIVE INHIBITORS; ADJUVANT TREATMENT; ESTROGEN-RECEPTOR; HIGHLY POTENT; DERIVATIVES; TAMOXIFEN; MECHANISM;

D O I：

10.1016/j.bioorg.2021.105017

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页数：27

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