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Review
. 2025 Mar 18.
doi: 10.1007/s11030-025-11160-3. Online ahead of print.

Recent progress and structural insights of potential Hsp90 inhibitors as anticancer agents

Affiliations
Review

Recent progress and structural insights of potential Hsp90 inhibitors as anticancer agents

Aastha Singh et al. Mol Divers. .

Abstract

Hsp90, or heat shock protein 90, a well-preserved molecular chaperone that is essential for the coordination of numerous biological pathways and cellular processes. Hsp90 is a molecular chaperone, which promises a target for cancer treatment. Hsp90 inhibitors are a class of drugs that have been extensively studied in preclinical models and demonstrated promise in treating a variety of illnesses, particularly cancer. Hsp90 inhibitors, however, have been encountered a number of challenges during the clinical development process, such as low efficacy, toxicity, and drug resistance. This literature survey emphasizes the importance of HSP90 inhibitors incorporating diverse heterocyclic rings, such as pyrazole, indole, pyrimidine, triazole, and thioquinazoline, which have exhibited promising anticancer activity. This review covers several parameters, including kinetic investigation, binding interactions, IC50 value, structure-activity relationship, and molecular docking studies of the most potent compound. There are several heterocyclic small molecules under investigation in clinical studies, such as AUY922, SNX-5422, STA-9090, and others. This review also contained a patent of HSP90 inhibitors, which showed greater effectiveness. Therefore, the main objective of this paper is to summarize all recent developments in the creation of anticancer medications that target HSP90 inhibitors in order to treat anticancer disease.

Keywords: Anticancer; HSP90; Indole; Pyrazole; Pyrimidine; Quinazoline; Structural activity relationship; Thioquinazoline.

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Conflict of interest statement

Declaration. Conflict of interest: The authors declare no competing interests. Ethical statement: Not applicable. Consent for publication: All of the authors are aware of and agree to the content of the paper and their being listed as a co-author of the paper.

References

    1. Russu WA (2015) Kinase inhibitors—targeted personalized cancer therapy. Updates on Cancer Treatment, pp 13–32.
    1. Bray F, Ferlay J, Soerjomataram I, Siegel RL, Torre LA, Jemal A (2018) Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin 68(6):394–424 - PubMed - DOI
    1. Eckhardt S (2002) Recent progress in the development of anticancer agents. Curr Med Chem Anticancer Agents 2(3):419–439 - PubMed - DOI
    1. Ali R, Mirza Z, Ashraf GM, Kamal MA, Ansari SA, Damanhouri GA, Abuzenadah AM, Chaudhary AG, Sheikh IA (2012) New anticancer agents: recent developments in tumor therapy. Anticancer Res 32(7):2999–3005 - PubMed
    1. Hoter A, El-Sabban ME, Naim HY (2018) The HSP90 family: structure, regulation, function, and implications in health and disease. Int J Mol Sci 19(9):2560 - PubMed - PMC - DOI

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