State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, P.R. China.
Mini Rev Med Chem. 2013 Nov;13(13):1957-66. doi: 10.2174/13895575113139990078.
Within the past years, many researches on the synthesis, structure-activity relationships (SAR), antitumor, antiinflammatory and anti-bacterial activities of the pyrazole derivatives have been reported. Several pyrazole derivatives possess important pharmacological activities and they have been proved useful materials in drug research. Pyrazole derivatives play an important role in antitumor agents because of their good inhibitory activity against BRAF(V600E), EGFR, telomerase, ROS Receptor Tyrosine Kinase and Aurora-A kinase. In addition, pyrazole derivatives also show good antiinflammatory and anti-bacterial activities. In this review, the bioactivities of the pyrazole derivatives mentioned above will be summarized in detail. We sincerely hope that increasing knowledge of the SAR and cellular processes underlying the bioactivity of pyrazole derivatives will be beneficial to the rational design of new generation of small molecule drugs.
在过去的几年中，已经有许多关于吡唑衍生物的合成、构效关系（SAR）、抗肿瘤、抗炎和抗菌活性的研究报告。一些吡唑衍生物具有重要的药理学活性，并且已被证明是药物研究中的有用材料。由于吡唑衍生物对 BRAF(V600E)、EGFR、端粒酶、ROS 受体酪氨酸激酶和 Aurora-A 激酶具有良好的抑制活性，因此它们在抗肿瘤药物中发挥着重要作用。此外，吡唑衍生物还表现出良好的抗炎和抗菌活性。在这篇综述中，将详细总结上述吡唑衍生物的生物活性。我们真诚地希望，对吡唑衍生物的生物活性的 SAR 和细胞过程的了解的增加将有助于新一代小分子药物的合理设计。
