Bozok University, Faculty of Arts and Sciences, Department of Chemistry, Yozgat, Turkey.
Bioorg Med Chem. 2013 Jul 1;21(13):3859-65. doi: 10.1016/j.bmc.2013.04.021. Epub 2013 Apr 19.
In this work novel organic based compounds, acyl thiourea derivatives were synthesized and their anticancer activities were investigated. A new series of acyl thiourea derivatives containing pyrazole ring were prepared in good yield through one pot reaction of 4-benzoyl-1, 5-diphenyl-1H-pyrazole-3-carbonyl chloride with ammonium thiocyanate and various amines. The structures of the newly synthesized compounds were confirmed by IR, (1)H NMR, (13)C NMR and elemental analysis. Anticancer activities of synthesized compounds were evaluated on human colon, liver and leukemia cancer cell lines. Cell culture studies have demonstrated significant toxicity of the compounds on the cell lines, and the levels of toxicity have altered in the presence of various side groups. These results confirm that novel pyrazolyl acyl thioureas derived compounds may be utilized for cancer treatment. Furthermore, these compounds have a great potential and significance for further investigations.
在这项工作中，合成了新型有机化合物——酰基硫脲衍生物，并研究了它们的抗癌活性。通过 4-苯甲酰基-1,5-二苯基-1H-吡唑-3-甲酰氯与硫氰酸铵和各种胺的一锅反应，以良好的产率制备了含有吡唑环的新系列酰基硫脲衍生物。新合成化合物的结构通过 IR、(1)H NMR、(13)C NMR 和元素分析得到确认。合成化合物的抗癌活性在人结肠、肝脏和白血病癌细胞系上进行了评估。细胞培养研究表明，这些化合物对细胞系具有显著的毒性，并且在存在各种侧基的情况下，毒性水平发生了改变。这些结果证实，新型吡唑基酰基硫脲衍生化合物可用于癌症治疗。此外，这些化合物具有进一步研究的巨大潜力和意义。
