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Research Progress of Diphenyl Urea Derivatives as Anticancer Agents and Synthetic Methodologies
Mini-Reviews in Organic Chemistry ( IF 2.3 ) Pub Date : 2019-11-30 , DOI: 10.2174/1570193x15666181029130418
Yi-Cong Wu 1 , Xin-Yue Ren 1 , Guo-Wu Rao 1
Affiliation  

The malignant neoplasm, which is recognized as cancer, is a serious threat to human health and frequently-occurring disease. Diphenylurea, an important link structure in the design of active substance for treating cancer due to its near-perfect binding with certain acceptors, has demonstrated many activities against several human cancer cell lines. Various novel compounds with diphenyl urea as anticancer agents were constructed with the successful development of sorafenib. Diphenylurea is utilized to treat cancer by inhibiting cell signaling transduction, such as RAS-RAFMEK- ERK signaling pathway and PI3K-Akt-mTOR pathway. In addition, this structure inhibits tumor cell growth by inhibiting receptor tyrosine kinases multiply, such as Vascular Endothelial Growth Factor Receptors (VEGFRs), Platelet-Derived Growth Factor Receptors (PDGFRs), Epidermal Growth Factor Receptors (EGFRs). It regulates the pH value in cells by inhibiting CAIX/XII and to achieve cancer therapeutic effect. Besides, the diphenyl urea structure is applied to the synthesis of reagents like Aurora kinases inhibitors and HDAC inhibitors that affect cell division and differentiation to treat cancer. To reach the goal of treating tumor, this structure is also used as a DNA-directed alkylating agent by affecting the expression of genes. An application of the most representative diphenyl urea derivatives as antitumor agents is summarized in this review, focusing on their mechanisms bound to the targets. Meanwhile, the progress of researches on methods of synthesizing diphenyl urea derivatives is provided.



中文翻译:

联苯尿素衍生物作为抗癌药及其合成方法的研究进展

恶性肿瘤被认为是癌症,是对人类健康和经常发生的疾病的严重威胁。由于联苯脲与某些受体的近乎完美结合,联苯脲是设计用于治疗癌症的活性物质中的重要链接结构,它已显示出针对几种人类癌细胞系的许多活性。随着索拉非尼的成功开发,构建了以二苯基脲为抗癌剂的各种新型化合物。通过抑制细胞信号转导,例如RAS-RAFMEK-ERK信号通路和PI3K-Akt-mTOR通路,联苯脲被用于治疗癌症。此外,该结构通过抑制受体酪氨酸激酶的倍增来抑制肿瘤细胞的生长,例如血管内皮生长因子受体(VEGFRs),血小板衍生生长因子受体(PDGFRs),表皮生长因子受体(EGFR)。它通过抑制CAIX / XII调节细胞的pH值,并达到癌症治疗效果。此外,二苯脲结构可用于合成影响细胞分裂和分化以治疗癌症的试剂,如Aurora激酶抑制剂和HDAC抑制剂。为了达到治疗肿瘤的目的,该结构还通过影响基因的表达而用作DNA定向的烷基化剂。这篇综述总结了最具代表性的二苯基脲衍生物作为抗肿瘤剂的应用,重点是它们与靶标结合的机制。同时,提供了合成二苯脲衍生物的方法的研究进展。它通过抑制CAIX / XII调节细胞的pH值,并达到癌症治疗效果。此外,二苯脲结构可用于合成影响细胞分裂和分化以治疗癌症的试剂,如Aurora激酶抑制剂和HDAC抑制剂。为了达到治疗肿瘤的目的,该结构还通过影响基因的表达而用作DNA定向的烷基化剂。这篇综述总结了最具代表性的二苯基脲衍生物作为抗肿瘤剂的应用,重点是它们与靶标结合的机制。同时,提供了合成二苯脲衍生物的方法的研究进展。它通过抑制CAIX / XII调节细胞的pH值,并达到癌症治疗效果。此外,二苯脲结构可用于合成影响细胞分裂和分化以治疗癌症的试剂,如Aurora激酶抑制剂和HDAC抑制剂。为了达到治疗肿瘤的目的,该结构还通过影响基因的表达而用作DNA定向的烷基化剂。这篇综述总结了最具代表性的二苯基脲衍生物作为抗肿瘤剂的应用,重点是它们与靶标结合的机制。同时,提供了合成二苯脲衍生物的方法的研究进展。二苯脲结构可用于合成影响细胞分裂和分化以治疗癌症的试剂,例如Aurora激酶抑制剂和HDAC抑制剂。为了达到治疗肿瘤的目的,该结构还通过影响基因的表达而用作DNA定向的烷基化剂。这篇综述总结了最具代表性的二苯基脲衍生物作为抗肿瘤剂的应用,重点是它们与靶标结合的机制。同时,提供了合成二苯脲衍生物的方法的研究进展。二苯脲结构可用于合成影响细胞分裂和分化以治疗癌症的试剂,例如Aurora激酶抑制剂和HDAC抑制剂。为了达到治疗肿瘤的目的,该结构还通过影响基因的表达而用作DNA定向的烷基化剂。这篇综述总结了最具代表性的二苯基脲衍生物作为抗肿瘤剂的应用,重点是它们与靶标结合的机制。同时,提供了合成二苯脲衍生物的方法的研究进展。这篇综述总结了最具代表性的二苯基脲衍生物作为抗肿瘤剂的应用,重点是它们与靶标结合的机制。同时,提供了合成二苯脲衍生物的方法的研究进展。这篇综述总结了最具代表性的二苯基脲衍生物作为抗肿瘤剂的应用,重点是它们与靶标结合的机制。同时,提供了合成二苯脲衍生物的方法的研究进展。

更新日期:2019-11-30
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