Abstract
This research has been successfully synthesized three compounds of 1,3,5-triaryl pyrazole derivatives by two steps reaction. Firstly, pyrazoline (4a-c) compound was obtained by one-pot reaction of aromatic ketones, aldehyde and hydrazine in basic condition. Then, pyrazole (5a-c) compound was obtained by oxidative aromatization of compound 4 in the presense of acetic acid. Chemical structure of predicted molecules was confirmed by FTIR, NMR and HRMS spectroscopy data analysis. Antiproliferative activity of compound 5a-c were evaluated by in vitro assay against MCF-7 cells line and molecular docking simulation against ERα (PDB ID: 3ERT) using MOE 2019. Biological evaluation result showed that pyrazole compounds had weak antiproliferative activity against MCF-7 cells with IC50 were > 1000 µM, whereas the docking studies agrees the result.
Highlights
Cancer is a major problem of health in both developed and developing countries
Estrogen receptor α (ERα) has been targeted for treatment of breast cancer cells using anti-estrogen compounds to block estrogenic signals, through a mechanism of competition against endogenous estrogens to bind to the receptors (Muchtaridi, Dermawan, & Yusuf, 2018)
Pyrazoline compounds prepared by one-pot synthesis method reported by Zamri, Teruna, Wulansari, Herfindo, & Ikhtiarudin, (2019), whereas aromatic substituted acetophenone, aromatic substituted benzaldehyde and phenylhydrazine were reacted in basic condition using sealed-vessel reactor at 80 ̊C to obtain pyrazoline 4a-c, followed by oxidative aromatization of pyrazoline in the presence of acetic acid to obtain pyrazole 5a-c compounds with good yields
Summary
Cancer is a major problem of health in both developed and developing countries. In 2018, 18.1 million cases of cancer were found, 9.6 million of which caused death, and are expected to continue to increase (Bray et al, 2018). Estrogen receptor α (ERα) is known to be responsible for the differentiation and proliferation of this breast cancer cells (Abdel-Hafiz, 2017). Despite its ability as an antagonist against breast cancer cells, about 40% of breast cancers that have previously responded to Tamoxifen, show intrinsic resistance (de novo resistance) (Badia, Oliva, Balaguer, & Cavailles, 2007). This has urged researcher to find a new generation of SERMs that were structurally different from their predecessors to avoid side effects, increase their specificity and activity
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