Title:Tetrazole Derivatives as Promising Anticancer Agents
VOLUME: 17 ISSUE: 14
Author(s):Elena A. Popova*, Aleksandra V. Protas and Rostislav E. Trifonov
Affiliation:Institute of Chemistry, Saint Petersburg State University, 7/9 Universitetskaya nab., Saint Petersburg, 199034, Institute of Chemistry, Saint Petersburg State University, 7/9 Universitetskaya nab., Saint Petersburg, 199034, Institute of Chemistry, Saint Petersburg State University, 7/9 Universitetskaya nab., Saint Petersburg, 199034
Keywords:Tetrazoles, anticancer agents, cancer, antitumor agents, coordination compounds, natural compounds.
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.
