Aryl- and Heteroaryl-Thiosemicarbazone Derivatives and Their Metal Complexes: A Pharmacological Template

• Tipo: Outra Publicação em Revista Científica Internacional
• Data: 2013

Autores

Narayana S H N Moorthy (Autor) Outra; Nuno M F S A Cerqueira (Autor) FCUP; Maria J Ramos (Autor) FCUP; Pedro A Fernandes (Autor) FCUP

Revista

Título: Recent Patents on Anti-Cancer Drug Discovery

Vol. 8

Páginas: 168-182

ISSN: 1574-8928

Editora: Bentham Science

Indexação

ISI Web of Knowledge - 46 Citações

Scopus - 48 Citações

Classificação Científica

FOS: Ciências médicas e da saúde > Medicina clínica

Outras Informações

ID Authenticus: P-005-0WN

DOI: 10.2174/157489213805290583

Abstract (EN): In this review, we discuss the current patents concerning aryl/heteroaryl thiosemicarbazone derivatives as regards to their activities and properties, including coordination (chelation) properties. The mode of action of the aryl/heteroaryl thiosemicarbazone derivatives involves metal coordination with proteins or biological fluids that have metal ions in their structure. Additionally, these molecules can also form multiple hydrogen bonds through their ( thio) amide and N3 nitrogen that ensure a strong interaction with the receptor. In some cases, strong pi-pi interactions can be observed too. Special attention is given to pyridyl, bis-pyridyl, benzoylpyridyl and isatin thiosemicarbazone derivatives that exhibit significant anticancer, antiviral and other activities in free and in metal complexed forms. This key biological role is often related with their capability to inhibit the enzyme ribonucleotide reductase, similar to what is observed with potent anticancer drugs such as Triapine and methisazone. Recent studies have revealed that thiosemicarbazone can also inhibit topoisomerase II alpha enzyme. Thiosemicarbazone derivatives form coordination complex with various metals such as Zn, Cu, Fe, Co, Ni, Pt, Pd, etc., and these complexes provide better activities than the free thiosemicarbazones. Recent patents show that the controlled or sustained release dosage form of the thiosemicarbazone derivatives along with ionizing radiations is used for the treatment of proliferative diseases (US20110152281, US20110245304, US20120172217).

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 15