School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou, 450001, PR China.
Department of Oncology, The Affiliated Cancer Hospital of Zhengzhou University, Henan Cancer Hospital, Henan Cancer Institute, NO.127, Dongming Road, Zhengzhou, 450008, PR China.
Eur J Med Chem. 2021 Mar 15;214:113218. doi: 10.1016/j.ejmech.2021.113218. Epub 2021 Jan 24.
Considerable progress has been made in the development of anticancer agents over the past few decades, and a lot of new anticancer agents from natural and synthetic sources have been produced. Among heterocyclic compounds, pyrimidine-fused bicyclic heterocycles possess a variety of biological activities such as anticancer, antiviral, etc. To date, 147 pyrimidine-fused bicyclic heterocycles have been approved for clinical assessment or are currently being used in clinic, 57 of which have been approved by FDA for clinical treatment of various diseases, and 22 of them are being used in the clinic for the treatment of different cancers. As the potentially privileged scaffolds, pyrimidine-fused bicyclic heterocycles may be used to discover new drugs with similar biological targets and improved therapeutic efficacy. This review aims to provide an overview of the anticancer applications and synthetic routes of 22 approved pyrimidine-fused bicyclic heterocyclic drugs in clinic.
在过去几十年中，抗癌药物的发展取得了相当大的进展，并且已经产生了许多来自天然和合成来源的新型抗癌药物。在杂环化合物中，嘧啶稠合双环杂环具有多种生物活性，如抗癌、抗病毒等。迄今为止，已有 147 种嘧啶稠合双环杂环化合物被批准进行临床评估或正在临床使用，其中 57 种已被 FDA 批准用于临床治疗各种疾病，22 种正在临床用于治疗不同类型的癌症。作为潜在的特权支架，嘧啶稠合双环杂环化合物可用于发现具有相似生物靶标和改善治疗效果的新药。本综述旨在概述 22 种已批准临床使用的嘧啶稠合双环杂环药物的抗癌应用和合成途径。
