最新药物设计策略和鉴定有望用于抗癌靶点的关键杂环支架

IF 12 1区 医学 Q1 PHARMACOLOGY & PHARMACY
Alia Mushtaq , Peng Wu , Muhammad Moazzam Naseer
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引用次数: 0

摘要

癌症是一种非传染性疾病,是全球死亡的主要原因,预计在未来二十年内将增加 75%,达到约 2 500 万例。放疗和手术等传统癌症治疗方法在降低癌症发病率方面效果有限。因此,癌症化疗的重点已转向开发新型小分子抗肿瘤药物,作为抗击和控制癌症发病率的另一种策略。杂环化合物就是这样一种制剂,它能与靶蛋白中的特定残基结合,抑制靶蛋白的功能,从而有可能治疗癌症。本综述重点介绍对碳酸酐酶和激酶(重要的抗癌靶标)具有强效活性的特异杂环药层。文章还讨论了正在进行的对各种恶性肿瘤具有潜在治疗价值的杂环化合物的临床前和临床研究评估,并简要概述了杂环支架在各种化疗方案中的作用。文章的主要目的是强调近期抗癌药物设计中涉及的关键杂环支架,这些支架需要药物开发界进一步关注,以找到更有效、更安全的靶向小分子抗癌药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Recent drug design strategies and identification of key heterocyclic scaffolds for promising anticancer targets

Recent drug design strategies and identification of key heterocyclic scaffolds for promising anticancer targets

Recent drug design strategies and identification of key heterocyclic scaffolds for promising anticancer targets

Cancer, a noncommunicable disease, is the leading cause of mortality worldwide and is anticipated to rise by 75% in the next two decades, reaching approximately 25 million cases. Traditional cancer treatments, such as radiotherapy and surgery, have shown limited success in reducing cancer incidence. As a result, the focus of cancer chemotherapy has switched to the development of novel small molecule antitumor agents as an alternate strategy for combating and managing cancer rates. Heterocyclic compounds are such agents that bind to specific residues in target proteins, inhibiting their function and potentially providing cancer treatment. This review focuses on privileged heterocyclic pharmacophores with potent activity against carbonic anhydrases and kinases, which are important anticancer targets. Evaluation of ongoing pre-clinical and clinical research of heterocyclic compounds with potential therapeutic value against a variety of malignancies as well as the provision of a concise summary of the role of heterocyclic scaffolds in various chemotherapy protocols have also been discussed. The main objective of the article is to highlight key heterocyclic scaffolds involved in recent anticancer drug design that demands further attention from the drug development community to find more effective and safer targeted small-molecule anticancer agents.

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来源期刊
CiteScore
23.00
自引率
0.70%
发文量
222
审稿时长
90 days
期刊介绍: Pharmacology & Therapeutics, in its 20th year, delivers lucid, critical, and authoritative reviews on current pharmacological topics.Articles, commissioned by the editor, follow specific author instructions.This journal maintains its scientific excellence and ranks among the top 10 most cited journals in pharmacology.
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