Institute of Chemistry, Saint Petersburg State University, 7/9 Universitetskaya nab., Saint Petersburg, 199034, Russian Federation.
Anticancer Agents Med Chem. 2018 Feb 7;17(14):1856-1868. doi: 10.2174/1871520617666170327143148.
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.
四唑环是一种有前途的药效团片段，常用于新型药物的开发。该部分是羧酸、顺酰胺和其他官能团的稳定、实际上不可代谢的生物等排体类似物。在过去的 10-15 年中，各种四唑的异构体（未取代的 NH、1H-取代和 2H-取代的四唑）已成功用于设计有前途的抗癌药物。含有四唑作为配体的过渡金属配位化合物、天然化合物（生物酸、肽、甾体、康普瑞汀等）的半合成四唑衍生物、5- 氧代和 5-硫代四唑以及一些其他相关化合物已被认为是有前途的抗肿瘤剂。本综述对这些四唑衍生物的合成及生物（抗癌）性质的现代方法进行了全面分析。挑选出了最有前途的用作抗癌剂的四唑结构类型。
