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Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil

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Roberto Parise-Filho

*Author for correspondence: Tel.: +55 113 091 3793;

E-mail Address: roberto.parise@usp.br

https://orcid.org/0000-0002-9311-7245

Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil

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Published Online:11 May 2022https://doi.org/10.4155/fmc-2021-0276

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Abstract

Cancer is the second most common cause of death worldwide. It can easily acquire resistance to treatments, demanding new therapeutic strategies, such as simultaneous inhibition of kinase and HDAC enzymes with hybrid inhibitors. Different approaches to this have varied according to their targets, with a few common trends, such as the usage of heterocycle scaffolds for kinase interaction, especially pyrimidine and quinazolines, and hydroxamic acids and benzamides for HDAC inhibition. Besides the hybrid compounds developed focusing on the inhibition tyrosine kinase and receptor tyrosine kinase, many advances have occurred in the development of serine-threonine kinase/HDAC and lipid kinase/HDAC novel compounds. Here, the latest strategies employed in this research area will be reviewed, alongside trends in inhibitor design, and observed gaps will be punctuated.

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Papers of special note have been highlighted as: • of interest; •• of considerable interest

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Vol. 14, No. 10

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Received 17 September 2021

Accepted 23 March 2022

Published online 11 May 2022

Published in print May 2022

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To view the supplementary data that accompany this paper please visit the journal website at: www.future-science.com/doi/suppl/10.4155/fmc-2021-0276

Acknowledgments

The authors are grateful to the Faculty of Pharmacy of University of São Paulo, which allowed the development of this work.

Conflict of interest

The authors declare no conflict of interest, financial or otherwise.

Financial & competing interests disclosure

The authors are grateful to Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) for financial support and grant #2021/08260-8 from São Paulo Research Foundation (FAPESP). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

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New kinase and HDAC hybrid inhibitors: recent advances and perspectives

Abstract

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References