Zhuang Chunlin, Zhang Wen, Sheng Chunquan, Zhang Wannian, Xing Chengguo, Miao Zhenyuan
School of Pharmacy, Second Military Medical University , 325 Guohe Road, Shanghai 200433, China.
School of Pharmacy, Ningxia Medical University , 1160 Shengli Street, Yinchuan 750004, China.
Chem Rev. 2017 Jun 28;117(12):7762-7810. doi: 10.1021/acs.chemrev.7b00020. Epub 2017 May 10.
Privileged structures have been widely used as an effective template in medicinal chemistry for drug discovery. Chalcone is a common simple scaffold found in many naturally occurring compounds. Many chalcone derivatives have also been prepared due to their convenient synthesis. These natural products and synthetic compounds have shown numerous interesting biological activities with clinical potentials against various diseases. This review aims to highlight the recent evidence of chalcone as a privileged scaffold in medicinal chemistry. Multiple aspects of chalcone will be summarized herein, including the isolation of novel chalcone derivatives, the development of new synthetic methodologies, the evaluation of their biological properties, and the exploration of the mechanisms of action as well as target identification. This review is expected to be a comprehensive, authoritative, and critical review of the chalcone template to the chemistry community.
特权结构作为药物发现中药物化学的有效模板已被广泛应用。查尔酮是许多天然化合物中常见的简单骨架。由于其合成简便，许多查尔酮衍生物也已被制备出来。这些天然产物和合成化合物已显示出众多有趣的生物活性，具有针对各种疾病的临床潜力。本综述旨在突出查尔酮作为药物化学中特权骨架的最新证据。本文将总结查尔酮的多个方面，包括新型查尔酮衍生物的分离、新合成方法的开发、其生物学性质的评估以及作用机制的探索和靶点鉴定。本综述有望成为化学界对查尔酮模板的全面、权威且批判性的综述。
