Synthesis and anticancer activity of acyl thioureas bearing pyrazole moiety
Synthesis and anticancer activity of acyl thioureas bearing pyrazole moiety
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DOI：
10.1016/j.bmc.2013.04.021
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发表时间：
2013-07-01
影响因子：
3.5
通讯作者：
Tutar, Yusuf
中科院分区：
文献类型：
--
作者：
Koca, Irfan;Ozgur, Aykut;Tutar, Yusuf
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-碳酰氯与硫氰酸铵和各种胺的一锅反应制备了一系列新的含吡唑环的酰基硫脲衍生物，收率良好。新合成的化合物的结构经IR、H-1 NMR、C-13 NMR和元素分析确证。在人结肠癌、肝癌和白血病癌细胞系上评估了合成化合物的抗癌活性。细胞培养研究表明这些化合物对细胞系具有显着毒性，并且毒性水平在各种侧基存在时发生变化。这些结果证实新型吡唑酰基硫脲衍生的化合物可用于癌症治疗。此外，这些化合物对于进一步研究具有巨大的潜力和意义。 (C)2013 Elsevier Ltd. 保留所有权利。
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, H-1 NMR, C-13 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. (C)2013 Elsevier Ltd. All rights reserved.