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杂环化合物:在抗癌药物发现中的重要性。

Heterocyclic Compounds: Importance in Anticancer Drug Discovery.

机构信息

Department of Biosciences and Biomedical Engineering, Indian Institute of Technology Indore, Simrol, Madhya Pradesh 453552, India.

Department of Chemistry, Institute of Science, Banaras Hindu University Varanasi, Uttar Pradesh 221005, India.

出版信息

Anticancer Agents Med Chem. 2022;22(19):3196-3207. doi: 10.2174/1871520622666220404082648.

Abstract

Cancer, a crucial global health problem, is characterized by abnormal cell division and uncontrolled growth. According to WHO, cancer is the second leading cause of global deaths and accounted for approximately 9.6 million deaths or one in six deaths in 2018. The National Cancer Registry Programme Report 2020, released by the ICMRIndia, estimated that there would be 13,90,000 cases of cancer in India in 2020 and that this number is likely to rise to 15,70,000 by 2025. In spite of several anti-cancer drugs, cancer cannot be cured completely, especially at late stages. In the current era, almost every person is suffering from some kind of disease. Thus, it is the necessity of time to develop novel, potent bioactive molecules. Many researchers are working on the development of new lead molecules or finding a new biological target for the betterment of human beings. However, heterocycles are constantly being used for the discovery of new lead molecules. Many of the clinically approved drugs contain the heterocyclic core as these molecules show exhilarating pharmaceutical properties, including anti-cancer agents such as methotrexate, vinblastine, vincristine, daunorubicin, 5-fluorouracil, doxorubicin, etc. Thus, heterocyclic compounds provide a fascinating research area for the design and development of anti-cancer drug(s). Herein, we focused on the natural as well as synthetic anti-cancer heterocyclic compounds. Furthermore, efforts have been made toward the mechanism of action of selected heterocyclic anti-cancer compounds.

摘要

癌症是一个严重的全球健康问题,其特征是细胞分裂异常和生长失控。根据世界卫生组织的数据,癌症是全球第二大致死原因,2018 年约有 960 万人死亡,占死亡总数的六分之一。印度医学研究理事会发布的《2020 年国家癌症登记计划报告》估计,2020 年印度癌症病例将达到 139 万例,到 2025 年这一数字可能上升到 157 万例。尽管有多种抗癌药物,但癌症仍无法完全治愈,尤其是在晚期。在当今时代,几乎每个人都患有某种疾病。因此,开发新型有效生物活性分子是当务之急。许多研究人员致力于开发新的先导分子或寻找新的生物靶标,以造福人类。然而,杂环化合物一直在被用于发现新的先导分子。许多已临床批准的药物都含有杂环核心,因为这些分子表现出令人振奋的药物特性,包括抗癌药物,如氨甲蝶呤、长春碱、长春新碱、柔红霉素、5-氟尿嘧啶、阿霉素等。因此,杂环化合物为设计和开发抗癌药物提供了一个引人入胜的研究领域。在此,我们重点介绍了天然和合成的抗癌杂环化合物。此外,还努力研究了选定的杂环抗癌化合物的作用机制。

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