嘌呤和嘧啶衍生物的抗癌潜力和结构活性研究:最新综述。

IF 3.8 2区 化学 Q2 CHEMISTRY, APPLIED
Tanushree Manna, Sumit Maji, Mousumi Maity, Biplab Debnath, Shambo Panda, Shah Alam Khan, Rajarshi Nath, Md Jawaid Akhtar
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引用次数: 0

摘要

癌症是世界头号死因,影响着全球数百万人的生命。过去几十年来,越来越多的研究都集中在开发新的抗癌药物上,但癌症仍然是一个全球性的健康挑战。因此,人们在药物设计和发现方面尝试了一些新的替代治疗策略。由于嘌呤和嘧啶杂环化合物在靶向各种癌症方面的潜力,它们最近受到了关注。从过去十年中最新发表的数据可以看出,在合成的衍生物中加入嘌呤和嘧啶环后,开发出了强效抗癌分子。本综述介绍了一些合成策略,包括最近开发的含嘌呤和嘧啶化合物作为抗癌剂的几个实例。此外,本文还介绍了它们的结构-活性关系,指出了增强抗癌活性所必需的片段或基团。嘌呤和嘧啶与其他杂环化合物的结合产生了许多新型抗癌分子,解决了耐药性的难题。嘌呤和嘧啶衍生物对靶向受体蛋白的抗癌活性明显增强,许多化合物的 IC50 值在纳摩尔范围内。这篇综述将为药物化学家提供支持,并有助于合成更有效的候选化疗药物,减轻这一可怕疾病的负担。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Anticancer potential and structure activity studies of purine and pyrimidine derivatives: an updated review

Anticancer potential and structure activity studies of purine and pyrimidine derivatives: an updated review

Anticancer potential and structure activity studies of purine and pyrimidine derivatives: an updated review

Cancer is the world’s leading cause of death impacting millions of lives globally. The increasing research over the past several decades has focused on the development of new anticancer drugs, but still cancer continues to be a global health challenge. Thus, several new alternative therapeutic strategies have been tried for the drug design and discovery. Purine and pyrimidine heterocyclic compounds have received attention recently due to their potential in targeting various cancers. It is evident from the recently published data over the last decade that incorporation of the purine and pyrimidine rings in the synthesized derivatives resulted in the development of potent anticancer molecules. This review presents synthetic strategies encompassing several examples of recently developed purine and pyrimidine-containing compounds as anticancer agents. In addition, their structure–activity relationships are represented in the schemes indicating the fragment or groups that are essential for the enhanced anticancer activities. Purine and pyrimidines combined with other heterocyclic compounds have resulted in many novel anticancer molecules that address the challenges of drug resistance. The purine and pyrimidine derivatives showed significantly enhanced anticancer activities against targeted receptor proteins with numerous compounds with an IC50 value in the nanomolar range. The review will support medicinal chemists and contribute in progression and development of synthesis of more potent chemotherapeutic drug candidates to mitigate the burden of this dreadful disease.

Graphical abstract

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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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