Article 2021 · 5 citations

Synthesis and biological evaluation of 3,5-diaryl-pyrazole derivatives as potential antiprostate cancer agents

Anil, Derya, Caykoylu, Emine U., Sanli, Fatma, Gambacorta, Nicola, Karatas, Omer F., Nicolotti, Orazio, Algul, Oztekin, Burmaoglu, Serdar

Abstract

Prostate cancer is the most frequently diagnosed tumor in men and the second leading cause of cancer-associated mortality in most developed countries. 3,5-Diaryl substituted pyrazole derivatives (20-28) were prepared starting from related chalcones and biologically evaluated for in vitro growth inhibition activity against PC3 and DU145 human prostate cancer cell lines. Compounds 23, 26, and 28 were found to be more potent as compared to the other halogen-substituted derivatives. Especially, the 2-bromo-substituted pyrazole derivative (26) was found to be more potent against PC3 and DU145 cells. Epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor 2 (VEGFR2) are known to be expressed in DU145 and PC3 cancer cells. The binding mode of the most selective compound 26 toward EGFR and VEGFR2 was investigated by employing docking simulations based on GLIDE standard precision (-5.912 and -6.949 kcal/mol, respectively).

Keywords

Claisen-Schmidt molecular docking prostate cancer pyrazole structure-activity relationships PROSTATE CHALCONES DESIGN RESISTANCE DISCOVERY APOPTOSIS PYRAZOLES ANALOGS EGFR

WoS Categories

Chemistry, Medicinal Chemistry, Multidisciplinary Pharmacology & Pharmacy

Sustainable Development Goals

Good Health and Well-being

Citation

Journal: ARCHIV DER PHARMAZIE
Year: 2021
Volume: 354
Issue: 12
ISSN: 0365-6233
eISSN: 1521-4184
DOI: 10.1002/ardp.202100225
WoS UID: WOS:000691394400001

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