Derivatives of pyrazole-based compounds as prospective cancer agents.
Ramoba, Lesetja V. Nzondomyo, Wakopo J. Serala, Karabo Macharia, Lucy W. Biswas, Supratim Prince, Sharon Prince Malan, Frederick P. Alexander, Orbett T. Manicum, Amanda-Lee E.
Ramoba, Lesetja V.
Nzondomyo, Wakopo J.
Serala, Karabo
Macharia, Lucy W.
Biswas, Supratim
Prince, Sharon Prince
Malan, Frederick P.
Alexander, Orbett T.
Manicum, Amanda-Lee E.
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Abstract
Five pyrazole-based compounds, 3,5-dimethyl-1H-pyrazole, L1; 3,5-diphenyl-1H-pyrazole, L2; 3-(trifluoromethyl)-5-phenyl-1H-pyrazole, L3; 3-(trifluoromethyl)-5-methyl-1H-pyrazole, L4; and 3,5-ditert-butyl-1H-pyrazole, L5 were synthesized from a typical condensation reaction of β-diketone derivatives with hydrazine hydrate reagent and characterized using various spectroscopic techniques such as FT-IR, UV–vis, 1H and 13C NMR, and LC–MS spectroscopy. L1 was further analyzed by single-crystal X-ray diffraction, and the N1–N1′ bond distance was found to be 1.361(3) Å and correlated well with other pyrazole-based compounds. The short-term cytotoxicity of 10 μM pyrazole compounds (L1–L5) was evaluated against pancreatic (CFPAC-1 and PANC-1), breast (MDA-MB-231 and MCF-7), and cervical (CaSki and HeLa) cancer cell lines using the MTT cell viability assay. Cisplatin and gemcitabine were included as positive control drugs followed by the determination of the half-maximal effective concentrations of prospective compounds. L2 and L3, respectively, displayed moderate cytotoxicity against CFPAC-1 (61.7 ± 4.9 μM) and MCF-7 (81.48 ± 0.89 μM) cell lines.
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Date
2025-03-20
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American Chemical Society (ACS)
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3,5-dimethyl-1H-pyrazole, L1, 3,5-diphenyl-1H-pyrazole, L2, 3-(trifluoromethyl)-5-phenyl-1H-pyrazole, L3, 3-(trifluoromethyl)-5-methyl-1H-pyrazole L4;, 3,5-ditert-butyl-1H-pyrazole, L5