{"title":"Recent progress in the development of HSP90 inhibitors: structure-activity relationship and biological evaluation studies.","authors":"Ankush Kumar, Aman Rai, Naresh Kumar Rangra, Thakur Gurjeet Singh, Samson Chibuzo Ugwuagbo, Rohit Bhatia","doi":"10.1007/s11030-025-11314-3","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":708,"journal":{"name":"Molecular Diversity","volume":" ","pages":""},"PeriodicalIF":3.8000,"publicationDate":"2025-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecular Diversity","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1007/s11030-025-11314-3","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
引用次数: 0
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.
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;