Abstract
Within the past ten years, a huge volume of research on the synthesis, structure-activity relationships (SAR), and anticancer activities of the urea derivatives was reported. Many aromatic urea derivatives such as N-phenyl-N-(2-chloroethyl)ureas (CEUs) and benzoylureas (BUs) show good anticancer activity, and these compounds have mainly been proved to be tubulin ligands that inhibit the polymerization of tubulin. Heterocyclic urea derivatives play an important role in anticancer agents because of their good inhibitory activity against receptor tyrosine kinases (RTKs), raf kinases, protein tyrosine kinases (PTKs), and NADH oxidase, which play critical roles in many aspects of tumorigenesis. Thiourea derivatives are also of wide interest because of their diverse anticancer activity against various leukemias and solid tumors. In this review, the anticancer activity of the urea derivatives mentioned above is summarized in detail. It is hoped that increasing knowledge of the SAR and cellular processes underlying the antitumor-activity of urea derivatives will be beneficial to the rational design of new generation of urea anticancer drugs.
Keywords: Urea derivatives, anticancer agents, heterocyclicureas, aromatic ureas, thiourea, structure-activity relationships
Anti-Cancer Agents in Medicinal Chemistry
Title: Urea Derivatives as Anticancer Agents
Volume: 9 Issue: 4
Author(s): Huan-Qiu Li, Peng-Cheng Lv, Tao Yan and Hai-Liang Zhu
Affiliation:
Keywords: Urea derivatives, anticancer agents, heterocyclicureas, aromatic ureas, thiourea, structure-activity relationships
Abstract: Within the past ten years, a huge volume of research on the synthesis, structure-activity relationships (SAR), and anticancer activities of the urea derivatives was reported. Many aromatic urea derivatives such as N-phenyl-N-(2-chloroethyl)ureas (CEUs) and benzoylureas (BUs) show good anticancer activity, and these compounds have mainly been proved to be tubulin ligands that inhibit the polymerization of tubulin. Heterocyclic urea derivatives play an important role in anticancer agents because of their good inhibitory activity against receptor tyrosine kinases (RTKs), raf kinases, protein tyrosine kinases (PTKs), and NADH oxidase, which play critical roles in many aspects of tumorigenesis. Thiourea derivatives are also of wide interest because of their diverse anticancer activity against various leukemias and solid tumors. In this review, the anticancer activity of the urea derivatives mentioned above is summarized in detail. It is hoped that increasing knowledge of the SAR and cellular processes underlying the antitumor-activity of urea derivatives will be beneficial to the rational design of new generation of urea anticancer drugs.
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Cite this article as:
Li Huan-Qiu, Lv Peng-Cheng, Yan Tao and Zhu Hai-Liang, Urea Derivatives as Anticancer Agents, Anti-Cancer Agents in Medicinal Chemistry 2009; 9 (4) . https://dx.doi.org/10.2174/1871520610909040471
DOI https://dx.doi.org/10.2174/1871520610909040471 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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