Chitkara College of Pharmacy, Chitkara University, Punjab, India.
Anticancer Agents Med Chem. 2020;20(18):2150-2168. doi: 10.2174/1871520620666200705214917.
Cancer is spreading all over the world, and it is becoming the leading cause of major deaths. Today's most difficult task for every researcher is to invent a new drug that can treat cancer with minimal side effects. Many factors, including pollution, modern lifestyle and food habits, exposure to oncogenic agents or radiations, enhanced industrialization, etc. can cause cancer. Treatment of cancer is done by various methods that include chemotherapy, radiotherapy, surgery and immunotherapy in combination or singly along with kinase inhibitors. Most of the anti-cancer drugs use the concept of kinase inhibition.
The number of drugs being used in chemotherapy has heterocycles as their basic structure in spite of various side effects. Medicinal chemists are focusing on nitrogen-containing heterocyclic compounds like pyrrole, pyrrolidine, pyridine, imidazole, pyrimidines, pyrazole, indole, quinoline, oxadiazole, azole, benzimidazole, etc. as the key building blocks to develop active biological compounds. The aim of this study is to attempt to compile a dataset of nitrogen-containing heterocyclic anti-cancer drugs.
We adopted a structural search on notorious journal publication websites and electronic databases such as Bentham Science, Science Direct, PubMed, Scopus, USFDA, etc. for the collection of peer-reviewed research and review articles for the present review. The quality papers were retrieved, studied, categorized into different sections, analyzed and used for article writing.
As per FDA databases, nitrogen-based heterocycles in the drug design are almost 60% of unique small-molecule drugs. Some of the nitrogen-containing heterocyclic anti-cancer drugs are Axitinib, Bosutinib, Cediranib, Dasatanib (Sprycel®), Erlotinib (Tarceva®), Gefitinib (Iressa®), Imatinib (Gleevec®), Lapatinib (Tykerb ®), Linifanib, Sorafenib (Nexavar®), Sunitinib (Sutent®), Tivozanib, etc. In the present review, we shall focus on the overview of nitrogen-containing heterocyclic active compounds as anti-cancer agents.
癌症正在全球蔓延，成为主要死亡原因。如今，每个研究人员面临的最大难题是发明一种新的药物，这种药物能以最小的副作用治疗癌症。许多因素，包括污染、现代生活方式和饮食习惯、接触致癌剂或辐射、工业化加剧等，都可能导致癌症。癌症的治疗方法有很多种，包括化疗、放疗、手术和免疫疗法的联合或单独应用，以及激酶抑制剂。大多数抗癌药物都采用了激酶抑制的概念。
尽管存在各种副作用，化疗中使用的药物数量仍以杂环为其基本结构。药物化学家专注于含氮杂环化合物，如吡咯、吡咯烷、吡啶、咪唑、嘧啶、吡唑、吲哚、喹啉、恶二唑、唑、苯并咪唑等，作为开发活性生物化合物的关键构建块。本研究旨在尝试编制一个含氮杂环抗癌药物数据集。
我们在著名的期刊出版物网站和电子数据库（如 Bentham Science、Science Direct、PubMed、Scopus、USFDA 等）上进行了结构搜索，以收集同行评议的研究和综述文章。检索高质量的论文，进行研究、分类成不同的章节，进行分析并用于撰写文章。
根据 FDA 数据库，药物设计中的含氮杂环几乎占独特小分子药物的 60%。一些含氮杂环抗癌药物包括阿昔替尼、博舒替尼、西地尼布、达沙替尼（Sprycel®）、厄洛替尼（Tarceva®）、吉非替尼（Iressa®）、伊马替尼（Gleevec®）、拉帕替尼（Tykerb®）、来那替尼、索拉非尼（Nexavar®）、舒尼替尼（Sutent®）、替沃扎尼等。在本综述中，我们将重点介绍含氮杂环活性化合物作为抗癌剂的概述。
