作为小分子酪氨酸激酶抑制剂的取代吡唑啉衍生物的结构-活性关系。

IF 3.5 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Saleem Akbar, Subham Das, Aman Kumar Mahto, Rikeshwer Prasad Dewangan, Bahar Ahmed
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引用次数: 0

摘要

背景:酪氨酸激酶抑制剂(TKIs)以某些细胞信号通路为靶点,近年来已成为治疗癌症的一类前景看好的药物。由于其独特的结构和适应性强的化学性质,吡唑啉类化合物引起了有机化学家和药物化学家的极大兴趣。其卓越的 TKI 活性促使人们开始研究癌症化疗:我们的目标是开发出抑制酪氨酸激酶效果显著、伤害最小的药物,从而改善癌症的治疗过程:本综述汇编了近期文献来源的最新信息,包括体外、体内、批准药物、活跃的临床试验,以及与癌症治疗中用作小分子酪氨酸激酶抑制剂的各种吡唑啉类似物相关的结构-活性关系(SAR):本研究重点关注吡唑啉环及其衍生物作为酪氨酸激酶抑制剂的结构活性关系(SAR),并强调了当前的研究进展,包括专利、授权药物和正在进行临床试验的化合物:通过加强我们对这些化合物的了解,我们的目标是帮助药理学家、科学家和研究人员更轻松地利用吡唑啉支架设计和开发下一代抗癌药物。未来,基于吡唑啉的疗法将有巨大的发展潜力,为正在进行的抗癌斗争带来新的希望。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Structure-Activity Relationship of Substituted Pyrazoline Derivatives as Small Molecule Tyrosine Kinase Inhibitors.

Background: Tyrosine kinase inhibitors (TKIs) target certain cell signalling pathways, and have become a promising class of medications for the treatment of cancer in recent years. Because of their distinct structure and adaptable chemistry, pyrazolines have drawn a lot of interest from organic and medicinal chemists. Their exceptional TKI activity has prompted them to investigate chemotherapy for cancer.

Objective: We aim to develop agents that inhibit tyrosine kinases highly effective with the least amount of harm possible, perhaps improving the course of cancer treatment.

Methods: This review compiled current information from recent literature sources, includ-ing in vitro, in vivo, approved medications, active clinical trials, and the structure-activity relationships (SAR) linked to various pyrazoline analogues used as small-molecule Tyro-sine Kinase Inhibitors in cancer treatment.

Results: This study focuses on SAR inside the pyrazoline ring and its derivatives as TKIs, and it emphasizes current developments, including patents, authorized medications, and compounds in clinical trials.

Conclusion: By enhancing our understanding of these compounds, our goal is to aid in making the roles of pharmacologists, scientists, and researchers who are designing and developing next-generation anticancer drugs with pyrazoline scaffolds easier. The future holds immense potential for the continued evolution of pyrazoline-based therapies, offer-ing renewed hope in the ongoing battle against cancer.

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来源期刊
Current medicinal chemistry
Current medicinal chemistry 医学-生化与分子生物学
CiteScore
8.60
自引率
2.40%
发文量
468
审稿时长
3 months
期刊介绍: Aims & Scope Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews and guest edited thematic issues written by leaders in the field covering a range of the current topics in medicinal chemistry. The journal also publishes reviews on recent patents. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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