Affiliation:
1. Laboratório de Análises Bioquímicas e Citológicas (LABC) Departamento de Análises Faculdade de Farmácia Universidade Federal do Rio Grande do Sul (UFRGS) Av. Ipiranga 2752, Bairro Santana CEP 90610–000 Porto Alegre RS Brazil
2. Postgraduate Program in Pharmaceutical Sciences Universidade Federal do Rio Grande do Sul (UFRGS) Av. Ipiranga 2752, Bairro Santana CEP 90610–000 Porto Alegre RS Brazil
Abstract
Abstract8‐Hydroxyquinoline and its derivatives consist of a group of metal‐binding ligands capable of reaching complexes that present several biological activities. In the present study, we collate and discuss data regarding the antileukemia activities of 8‐hydroxyquinoline (8HQ) compounds to provide an overview of their mechanisms of actions, and a compilation of cytotoxicity data against diverse leukemia cell lines. The pharmacological activities of this class of agents are associated primarily with their ability to coordinate metals and interact with multiple biological targets. We found consistent evidence that 8HQ exerts promising proapoptotic features through its direct interaction with deoxyribonucleic acid (DNA) and inhibition of multiple targets, such as the proteasome, nuclear factor kappa B (NF‐κB), histone deacetylase (HDAC), bromodomain and extra terminal (BET) proteins and janus kinases (JAKs), in addition to inducing autophagy associated cell death. Thus, we provide substantial evidence for the repositioning potential of the 8HQ class for the treatment of leukemia, a hematological malignancy for which urgent advances in therapeutic approaches are needed to overcome conventional therapy limitations.
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5 articles.
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