Derivatives of Pyrazole-Based Compounds as Prospective Cancer Agents
Lesetja V. Ramoba, Wakopo J. Nzondomyo, Karabo Serala, Lucy Wanjiku Macharia, Supratim Biswas, Sharon Prince, Frederick P. Malan, Orbett T. Alexander, Amanda‐Lee E. Manicum
Abstract
High Resolution Image Download MS PowerPoint Slide Five pyrazole-based compounds, 3,5-dimethyl-1 H -pyrazole, L1; 3,5-diphenyl-1 H -pyrazole, L2; 3-(trifluoromethyl)-5-phenyl-1 H -pyrazole, L3; 3-(trifluoromethyl)-5-methyl-1 H -pyrazole, L4; and 3,5-ditert-butyl-1 H -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, 1 H and 13 C 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.