Use of anastrozole in the chemoprevention and treatment of breast cancer: A literature review

Abstract

Aromatase inhibitors have emerged as an alternative endocrine therapy for the treatment of hormone sensitive breast cancer in postmenopausal women. The use of third-generation inhibitors represented by exemestane, letrozol and anastrozole is currently indicated. Anastrozole is a nonsteroidal compound and a potent selective inhibitor of the aromatase enzyme. Although a few studies have shown that its pharmacodynamic and pharmacokinetic properties may be affected by interindividual variability, this drug has been recently used in all configurations of breast cancer treatment. In metastatic disease, it is currently considered the first-line treatment for postmenopausal women with estrogen receptor-positive breast tumors. Anastrozole has shown promising results in the adjuvant treatment of early-stage breast cancer in postmenopausal women. It has also achieved interesting results in the chemoprevention of the disease. Therefore, due to the importance of anastrozole both for endocrine treatment and chemoprevention of hormone-sensitive breast cancer in postmenopausal women, we proposed the current literature review in the SciELO and PubMed database of articles published in the last 10 years.

The synthesis and the study of the antitumor activity of 3-R-6-(4-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine hydrobromides

“…Target 7H- [1,2,4]triazolo [3,4-b] [1,3,4]thiadiazine hydrobromides 3a -g were synthesized by the interaction of 4-amino-5-R-4H-1,2,4-triazole-3-thiols 2a -g with 4-methoxyphenacyl bromide with relatively high yields (Scheme). Starting triazoles 2b -g were obtained by the reaction of thiocarbohydrazide (1) with the corresponding carboxylic acids, for 5-unsubstituted triazole 2a formamide was used as a condensing reagent.…”

“…To determine the antineoplastic activity of 3-R-6-(4-methoxyphenyl)-7H- [1,2,4]triazolo [3,4-b] [1,3,4]thiadiazine hydrobromides 3 the in vitro study was conducted on 60 lines of cancer cells (leukemia, nonsmall cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer) according to the standard procedure of the mitotic activity assessment of new potential bioactive compounds by the fluorescent coloring method (sulforhodamine B as a dye) performed in the US National Cancer Institute within the Development Therapeutic Program [14]. The substances were used in the concentration of 10 -5 mol/L, cancer cells were incubated with the compounds for 48 hours.…”

“…The anti-tumor activity of 3-alkyl-6-(4-methoxyphenyl)-7H- [1,2,4]triazolo [3,4- At the second stage of the study the most active compounds 3c, 3f and 3g were tested in five concentrations in 10-fold dilution series (100 μm, 10 μm, 1 μm, 0.1 μm and 0.01 μm) on the lines of human can-cer cells listed above. As a result of the experiment, three dose-dependent parameters were calculated: the GI 50 value (the growth inhibitory activity, effective inhibition level) corresponded to the concentration of the compound causing 50 % decrease in the net cell growth, the TGI value (cytostatic activity) -the concentration of the compound resulting in the total growth inhibition (TGI), and the LC 50 value (cytotoxic activity)the concentration of the compound causing a net 50 % loss of initial cells at the end of the incubation period.…”

“…It is also known that derivatives of triazole and thiadiazine demonstrate a wide range of biological effects [8 -10]. On the other hand, derivatives of 7H- [1,2,4]triazolo [3,4-b] [1,3,4]thiadiazine exhibit the antimicrobial, antifungal activity [11][12] and anti-inflammatory activity [13].…”

The Potential Mechanism of Bufadienolide-Like Chemicals on Breast Cancer via Bioinformatics Analysis

“…Valproic acid, a histone deacetylase inhibitor, which once was widely used as an antiepileptic, has recently also shown anti-cancer activity in an vitro/vivo model [25]. Estradiol is a sex hormone with anticancer activity, and is also widely used for the treatment of breast cancer, especially for postmenopausal women [26,27,28].…”