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Multi-target compounds acting in cancer progression: Focus on thiosemicarbazone, thiazole and thiazolidinone

Lucianna Rabelo Pessoa de Siqueira¹, Paulo André Teixeira de Moraes Gomes², Larissa Pelágia de Lima Ferreira¹

¹Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Pernambuco, 50740-520, Recife, PE, Brazil; Universidade Federal de Pernambuco, Laboratório de Imunomodulação e Novas Abordagens Terapêuticas, Núcleo de Pesquisas Em Inovação Terapêutica Suely Galdino, Recife, Pernambuco, Brazil.

European Journal of Medicinal Chemistry

|March 25, 2019

Abstract:

Currently, cancer and its progression to metastasis result in a large number of deaths. The lack of new drugs, appropriate clinical trials for metastasis preventive drugs and incomplete understanding of the molecular machinery are the major obstacles in metastasis prevention and treatment. On the other hand, thiosemicarbazones and their bioisosteres, thiazole and thiazolidinone are recurring in a wide range of biologically active compounds that reach different targets within tumor context and represent a promising start point to access potential candidates in metastatic cancer. Therefore, the search for new lead compounds showing highest anticancer potency and less adverse effects is the major challenger in drug discovery. The search was based from 1994 to 2018, focusing on thiosemicarbazone, thiazole and thiazolidinone cores that allowed us to discuss how the three multi-target motifs have been used for the target-based design and development of anticancer agents. In the lasts years, thiosemicarbazone, thiazole, and thiazolidinone cores are recurrent in many approaches for cancer therapy. In our search, it was verified that due to its biodiversity and versatility the anticancer potential of such structures has been assigned to distinct mechanisms reinforcing the value of these cores in the anticancer drug development. The present article aims point out the current application of thiosemicarbazone, thiazole and thiazolidinone cores in the design of anticancer agents within tumor progression, acting via varied targets such as cathepsins, NDRG1 gene and kinases, showing in vitro tests, in vivo tests and clinical trials. In our search it was possible to verify that thiazole is the most studied and the most important of the three structures. Therefore, we hope to provide new insights and valuable inspiration in the research of new drugs and development and contribute to the management of cancer.

Insights

New anticancer drug discovery focuses on thiosemicarbazone, thiazole, and thiazolidinone compounds. Thiazole-based agents show the most promise for treating metastatic cancer by targeting multiple tumor pathways.

Area of Science:

Medicinal Chemistry
Oncology
Drug Discovery

Background:

Metastatic cancer remains a leading cause of death, with limited treatment options and a poor understanding of its molecular mechanisms.
Thiosemicarbazones, thiazoles, and thiazolidinones are heterocyclic compounds with diverse biological activities relevant to cancer therapy.
Developing novel anticancer agents with high potency and reduced side effects is a critical challenge in drug discovery.

Purpose of the Study:

To review the application of thiosemicarbazone, thiazole, and thiazolidinone cores in the design of anticancer agents.
To highlight the multi-target mechanisms of these compounds against tumor progression.
To identify promising lead compounds for metastatic cancer treatment.

Main Methods:

Literature search from 1994 to 2018 focusing on thiosemicarbazone, thiazole, and thiazolidinone derivatives.
Analysis of target-based drug design strategies utilizing these heterocyclic cores.
Evaluation of in vitro, in vivo, and clinical trial data for anticancer efficacy.

Main Results:

Thiosemicarbazone, thiazole, and thiazolidinone cores are versatile scaffolds for developing multi-target anticancer agents.
These compounds act on various targets, including cathepsins, NDRG1 gene, and kinases.
Thiazole emerged as the most extensively studied and significant scaffold among the three.

Conclusions:

Thiosemicarbazone, thiazole, and thiazolidinone derivatives represent a valuable resource for anticancer drug development.
Their diverse mechanisms of action offer potential for overcoming treatment resistance in metastatic cancer.
Further research into these scaffolds can provide new insights and inspire the development of novel cancer therapeutics.

Read full analysis

Keywords:

Anticancer Heterocyclic Metastasis Thiazole Thiazolidinone Thiosemicarbazone

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