Recent progress in the development of HSP90 inhibitors: structure-activity relationship and biological evaluation studies.

IF 3.8 2区 化学 Q2 CHEMISTRY, APPLIED
Ankush Kumar, Aman Rai, Naresh Kumar Rangra, Thakur Gurjeet Singh, Samson Chibuzo Ugwuagbo, Rohit Bhatia
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Abstract

In cellular biology, Heat Shock Protein 90 (Hsp90) plays a pivotal role in coordinating several processes essential or cellular survival, cell signaling and other processes. This analysis explores the complex structure, biological significance, and regulatory mechanisms clarifying its essential function in preserving cellular homeostasis and its relevance in a range of illnesses, such as cancer, neurological conditions, infectious diseases, cardiovascular conditions, and autoimmune diseases. Hsp90 is a prominent target for cancer treatment. The current manuscript involved the recent progress in the synthesis and development of Hsp90 inhibitor for the treatment of cancer. In this manuscript, the authors have compiled the Hsp90 inhibitors containing various heterocyclic rings such as Benzothiazone, Benzamide, Isoxazole, Pyrimidinone, Imidazole, Pyrimidine, Isatin, Quinazoline and Pyrazole etc. In this review, the authors incorporate the anticancer activity, Structure-Activity Relationship (SAR), Molecular Docking studies and Biological Evaluation of recently synthesized Hsp90 inhibitors. The authors have also added the clinical trial status of Hsp90 inhibitors and their potential use in cancer therapy. Overall, this review highlights the recent advancements in the field of Hsp90 inhibitor from 2020 to present. This review provides medicinal chemists with comprehensive insights into the development of Hsp90 inhibitors by guiding future research and drug discovery efforts in cancer.

HSP90抑制剂的研究进展:构效关系及生物学评价研究。
在细胞生物学中,热休克蛋白90 (Heat Shock Protein 90, Hsp90)在协调细胞存活、细胞信号传导等过程中起着关键作用。本分析探讨了其复杂的结构、生物学意义和调节机制,阐明了其在维持细胞稳态中的基本功能,以及在一系列疾病(如癌症、神经系统疾病、传染病、心血管疾病和自身免疫性疾病)中的相关性。Hsp90是癌症治疗的重要靶点。目前的稿件涉及治疗癌症的Hsp90抑制剂的合成和开发的最新进展。本文对含苯并噻唑、苯甲酰胺、异恶唑、嘧啶酮、咪唑、嘧啶、Isatin、喹唑啉、吡唑等多种杂环的Hsp90抑制剂进行了整理。本文就近年来合成的Hsp90抑制剂的抗癌活性、构效关系、分子对接研究和生物学评价等方面进行综述。作者还补充了Hsp90抑制剂的临床试验状态及其在癌症治疗中的潜在应用。总的来说,本文综述了从2020年到现在Hsp90抑制剂领域的最新进展。这篇综述为药物化学家提供了对Hsp90抑制剂开发的全面见解,指导了未来在癌症中的研究和药物发现工作。
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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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