Prachayasittikul Supaluk, Pingaew Ratchanok, Worachartcheewan Apilak, Sinthupoom Nujarin, Prachayasittikul Veda, Ruchirawat Somsak, Prachayasittikul Virapong
Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand.
Department of Chemistry, Faculty of Science, Srinakharinwirot University, Bangkok 10110, Thailand.
Mini Rev Med Chem. 2017;17(10):869-901. doi: 10.2174/1389557516666160923125801.
Cancer has been considered to be a global health concern due to the impact of disease on the quality of life. The continual increase of cancer cases as well as the resistance of cancer cells to the existing drugs have driven the search for novel anticancer drugs with better potency and selectivity, improved pharmacokinetic profiles, and minimum toxicities. Pyridine and pyrimidine are presented in natural products and genetic materials. These pyridine/pyrimidine core structures have been noted for their roles in many biological processes as well as in cancer pathogenesis, which make such compounds become attractive scaffolds for discovery of novel drugs.
RESULTS & CONCLUSION: In the recent years, pyridine- and pyrimidine-based anticancer drugs have been developed based on structural modification of these core structures (i.e., substitution with moieties and rings, conjugation with other compounds, and coordination with metal ions). Detailed discussion is provided in this review to highlight the potential of these small molecules as privileged scaffolds with attractive properties and biological activities for the search of novel anticancer agents.
由于癌症对生活质量的影响,它已被视为一个全球健康问题。癌症病例的持续增加以及癌细胞对现有药物的耐药性,促使人们寻找具有更高效力和选择性、改善的药代动力学特征以及最小毒性的新型抗癌药物。吡啶和嘧啶存在于天然产物和遗传物质中。这些吡啶/嘧啶核心结构因其在许多生物过程以及癌症发病机制中的作用而受到关注,这使得此类化合物成为发现新型药物的有吸引力的骨架。
近年来已基于这些核心结构的结构修饰(即,用基团和环进行取代、与其他化合物共轭以及与金属离子配位)开发了基于吡啶和嘧啶的抗癌药物。本综述提供了详细讨论,以突出这些小分子作为具有吸引人的性质和生物活性的特权骨架在寻找新型抗癌剂方面的潜力。