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

• Type: Another Publication in an International Scientific Journal
• Date: 2013

Authors

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

Journal

Title: Recent Patents on Anti-Cancer Drug Discovery

Vol. 8

Pages: 168-182

ISSN: 1574-8928

Publisher: Bentham Science

Indexing

ISI Web of Knowledge - 46 Citations

Scopus - 48 Citations

Scientific classification

FOS: Medical and Health sciences > Clinical medicine

Other information

Authenticus ID: 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).

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 15