Journal
ARABIAN JOURNAL OF CHEMISTRY
Volume 12, Issue 6, Pages 816-824Publisher
ELSEVIER
DOI: 10.1016/j.arabjc.2015.12.006
Keywords
Aminopyrazole; Thiourea; G2/M arrest; Apoptosis
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Funding
- European Social Fund for Sectoral Operational Programme Human Resources Development 2007-2013 [POSDRU/159/1.5/S/135760]
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We designed new pyrazole derivatives as inhibitors of the cell cycle kinases and developed a simple environmentally sustainable synthesis process. We synthesized the pyrazolyl thiourea derivatives using rapid ultrasound mediated methods and confirmed their structures by NMR and IR spectra. The apoptosis and necrosis inducing effects of the new compounds were investigated. Cell cycle analysis and expression of genes involved in apoptosis, cell cycle and xenobiotic metabolism were studied. The compounds presented modest apoptotic effects in human cancer cells. The N-[[3-(4-bromophenyl)-1H-pyrazol-5-yl]carbamothioy1]-4-chloro-benzamide compound (4e) induced a significant increase of cells in G2/M phases in conjunction with an increased expression of cyclin A and cyclin B, emerging as a promising anticancer drug, to be further developed in animal models of cancer. (C) 2015 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.
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