Tetrazole Derivatives as Promising Anticancer Agents

Author(s): Elena A. Popova*, Aleksandra V. Protas, Rostislav E. Trifonov

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 17 , Issue 14 , 2017

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Graphical Abstract:


Tetrazole cycle is a promising pharmacophore fragment frequently used in the development of novel drugs. This moiety is a stable, practically non-metabolized bioisosteric analog of carboxylic, cis-amide, and other functional groups. Over recent 10–15 years, various isomeric forms of tetrazole (NH-unsubstituted, 1H-1- substituted, and 2H-2-substituted tetrazoles) have been successfully used in the design of promising anticancer drugs. Coordination compounds of transition metals containing tetrazoles as ligands, semisynthetic tetrazolyl derivatives of natural compounds (biogenic acids, peptides, steroids, combretastatin, etc.), 5-oxo and 5- thiotetrazoles, and some other related compounds have been recognized as promising antineoplastic agents. This review presents a comprehensive analysis of modern approaches to synthesis of these tetrazole derivatives as well as their biological (anticancer) properties. The most promising structure types of tetrazoles to be used as anticancer agents have been picked out.

Keywords: Tetrazoles, anticancer agents, cancer, antitumor agents, coordination compounds, natural compounds.

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Article Details

Year: 2017
Published on: 27 March, 2017
Page: [1856 - 1868]
Pages: 13
DOI: 10.2174/1871520617666170327143148
Price: $65

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