Recent Developments and Structure–Activity Relationships of BRAF Inhibitors for Cancer Drug Discovery

IF 3.5 3区 医学 Q2 CHEMISTRY, MEDICINAL
Xin-Ke Guo, Kadalipura P. Rakesh, Sahana Raju, Kothanahally S. Sharath Kumar, Hua-Li Qin
{"title":"Recent Developments and Structure–Activity Relationships of BRAF Inhibitors for Cancer Drug Discovery","authors":"Xin-Ke Guo,&nbsp;Kadalipura P. Rakesh,&nbsp;Sahana Raju,&nbsp;Kothanahally S. Sharath Kumar,&nbsp;Hua-Li Qin","doi":"10.1002/ardp.70322","DOIUrl":null,"url":null,"abstract":"<div>\n \n <p>Incorporating current structural and biochemical discoveries, this paper examines how B-RAF inhibitors control B-RAF, including their clinical efficacy, side effects, and important medicinal chemistry characteristics. It investigates the molecular insights that may direct the creation of more potent RAF inhibitors that can target different oncogenic B-RAF conformations. We have discussed the advantages and disadvantages of structurally varied next-generation RAF inhibitors that are presently undergoing preclinical and clinical trials. A few of these drug candidates have started clinical trials with promising outcomes. This review also covers the structure–activity relationship of promising bioactive B-RAF compounds, highlights advancements in the discovery and development of B-RAF inhibitors, and attempts to assist future drug discovery initiatives.</p></div>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"359 8","pages":""},"PeriodicalIF":3.5000,"publicationDate":"2026-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Archiv der Pharmazie","FirstCategoryId":"3","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/ardp.70322","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0

Abstract

Incorporating current structural and biochemical discoveries, this paper examines how B-RAF inhibitors control B-RAF, including their clinical efficacy, side effects, and important medicinal chemistry characteristics. It investigates the molecular insights that may direct the creation of more potent RAF inhibitors that can target different oncogenic B-RAF conformations. We have discussed the advantages and disadvantages of structurally varied next-generation RAF inhibitors that are presently undergoing preclinical and clinical trials. A few of these drug candidates have started clinical trials with promising outcomes. This review also covers the structure–activity relationship of promising bioactive B-RAF compounds, highlights advancements in the discovery and development of B-RAF inhibitors, and attempts to assist future drug discovery initiatives.

BRAF抑制剂在癌症药物开发中的最新进展及构效关系
结合目前的结构和生化发现,本文研究了B-RAF抑制剂如何控制B-RAF,包括它们的临床疗效、副作用和重要的药物化学特征。它调查了可能指导创造更有效的RAF抑制剂的分子见解,这些抑制剂可以针对不同的致癌B-RAF构象。我们已经讨论了结构不同的下一代RAF抑制剂的优缺点,这些抑制剂目前正在进行临床前和临床试验。其中一些候选药物已经开始临床试验,结果很有希望。本综述还涵盖了具有生物活性的B-RAF化合物的构效关系,重点介绍了B-RAF抑制剂的发现和开发进展,并试图协助未来的药物发现计划。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
Archiv der Pharmazie
Archiv der Pharmazie 医学-化学综合
CiteScore
7.90
自引率
5.90%
发文量
176
审稿时长
3.0 months
期刊介绍: Archiv der Pharmazie - Chemistry in Life Sciences is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry. Emphasis is put on papers combining synthetic organic chemistry, structural biology, molecular modelling, bioorganic chemistry, natural products chemistry, biochemistry or analytical methods with pharmaceutical or medicinal aspects such as biological activity. The focus of this journal is put on original research papers, but other scientifically valuable contributions (e.g. reviews, minireviews, highlights, symposia contributions, discussions, and essays) are also welcome.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信
小红书