Derivatives of Pyrazole-Based Compounds as Prospective Cancer Agents

Five pyrazole-based compounds, 3,5-dimethyl-1<i>H</i>-pyrazole, <b>L1</b>; 3,5-diphenyl-1<i>H</i>-pyrazole, <b>L2</b>; 3-(trifluoromethyl)-5-phenyl-1<i>H</i>-pyrazole, <b>L3</b>; 3-(trifluoromethyl)-5-methyl-1<i>H</i>-pyrazole, <b>L4</b>; and 3,5-ditert-butyl-1<i>H</i>-pyrazole, <b>L5</b> 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. <b>L1</b> 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 (<b>L1</b>-<b>L5</b>) 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. <b>L2</b> and <b>L3</b>, respectively, displayed moderate cytotoxicity against CFPAC-1 (61.7 ± 4.9 μM) and MCF-7 (81.48 ± 0.89 μM) cell lines.