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.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bioorg.2021.105017 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Spontaneous regression in breast cancer is rare but can dramatically improve patient prognosis. Although the underlying mechanism is unknown, it may be due to a biological response to external invasion. An 81-year-old woman presented to our emergency department with a 600x100mm large breast mass.
View Article and Find Full Text PDFMusculoskeletal symptoms associated with aromatase inhibitors in the treatment of early breast cancer: A scoping review of risk factors and outcomes.
Support Care Cancer
January 2025
Fudan University School of Nursing, Shanghai, China and Fudan University Centre for Evidence-Based Nursing: A Joanna Briggs Institute Centre of Excellence, 305 Fenglin Rd, Shanghai, 200032, China.
Purpose: Aromatase inhibitor-associated musculoskeletal symptoms (AIMSS) are the most common adverse effects experienced by breast cancer patients. This scoping review aimed to systematically synthesize the predictors/risk factors and outcomes of AIMSS in patients with early-stage breast cancer.
Methods: A systematic search was conducted in PubMed, Web of Science, EMBASE, CINAHL, and the China National Knowledge Internet (CNKI) from inception to December 2024 following the scoping review framework proposed by Arksey and O'Malley (2005).
New Promising Steroidal Aromatase Inhibitors with Multi-Target Action on Estrogen and Androgen Receptors for Breast Cancer Treatment.
Cancers (Basel)
January 2025
UCIBIO-Applied Molecular Biosciences Unit, Laboratory of Biochemistry, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, n° 228, 4050-313 Porto, Portugal.
Endocrine therapies that comprise anti-estrogens and aromatase inhibitors (AIs) are the standard treatment for estrogen receptor-positive (ER+) (Luminal A) breast cancer-the most prevalent subtype. However, the emergence of resistance restricts their success by causing tumor relapse and re-growth, which demands a switch towards other therapeutic approaches in order to minimize or overcome resistance. Indeed, this clinical limitation highlights the search for new molecules to improve cancer treatment.
View Article and Find Full Text PDFThe efficacy and safety of rhGH treatment combined with letrozole/GnRHa in adolescent boys.
BMC Pediatr
January 2025
Department of Endocrinology, Genetics and Metabolism, Fuzhou First General Hospital Affiliated with Fujian Medical University, Fuzhou Children's Hospital of Fujian Medical University, Fuzhou, 350005, China.
Objective: In boys during puberty who were undergoing recombinant human growth hormone (rhGH) treatment, we compared the therapeutic efficacy on growth, and any adverse reactions, of co-therapy with either letrozole or gonadotropin-releasing hormone analog (GnRHa).
Methods: Fifty-six pubertal growth hormone deficiency (GHD) boys were studied, they were treated with the combination of letrozole and rhGH (letrozole group, n = 28) or the combination of GnRHa and rhGH (GnRHa group, n = 28) for at least one year. Eighteen patients in the letrozole group and seventeen patients in the GnRHa group attained final adult height (FAH).
Safety of topical estrogen therapy during adjuvant endocrine treatment among patients with breast cancer: A meta-analysis based expert panel discussion.
Cancer Treat Rev
January 2025
Department of Oncology, Faculty of Medicine and Health, Örebro University, Örebro, Sweden. Electronic address:
Importance: Endocrine treatments, such as Tamoxifen (TAM) and/or Aromatase inhibitors (AI), are the adjuvant therapy of choice for hormone-receptor positive breast cancer. These agents are associated with menopausal symptoms, adversely affecting drug compliance. Topical estrogen (TE) has been proposed for symptom management, given its' local application and presumed reduced bioavailability, however its oncological safety remains uncertain.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!