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.

Water soluble Pd(ii) and Pt(ii)–ADC species synthesized via the metal-mediated coupling of isocyanides and 1,2-diaminobenzene have demonstrated antitumor potential.

No abstract

A series of tris(5‐aryl‐1H‐tetrazol‐1‐yl)methanes (3a‐3g) and 2‐dichloromethyl‐5‐aryl‐2H‐tetrazoles (4a‐4d) were synthesized by reaction of 5‐aryl‐NH‐tetrazoles with trichloromethane in strong aqueous basic condition. The compounds obtained were fully characterized by means of HRESI‐MS, 1H and 13C{1H} NMR spectroscopies, as well as by single‐crystal X‐ray diffraction (for 3a, 3b, 4d). Inspection of the X‐ray diffraction data and Hirshfeld surface analysis for tris(5‐aryl‐1H‐tetrazol‐1‐yl)methanes 3a,b and 2‐dichloromethyl‐5‐aryl‐2H‐tetrazole 4d showed the presence of noncovalent π‐hole•••lone pair and π‐hole•••π interactions involving electrophilic tetrazole carbon atom.

No abstract