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It is now well known as a bioisostere for various functions, such as the amide or the ester bond, positioning it as a key pharmacophore in medicinal chemistry and it has found applications in various fields including life sciences. Attention was first focused on the synthesis of 1,4\u2010disubstituted 1,2,3\u2010triazole molecules however 1,4,5\u2010trisubstituted 1,2,3\u2010triazoles have now emerged as valuable molecules due to the possibility to expand the structural modularity. In the last decade, methods mainly derived from the copper(I)\u2010catalyzed azide\u2010alkyne cycloaddition (CuAAC) reaction have been developed to access halo\u2010triazole compounds and have been applied to nucleosides, carbohydrates, peptides and proteins. In addition, late\u2010stage modification of halo\u2010triazole derivatives by metal\u2010mediated cross\u2010coupling or halo\u2010exchange reactions offer the possibility to access highly functionalized molecules that can be used as tools for chemical biology. This review summarizes the synthesis, the functionalization, and the applications of 1,4,5\u2010trisubstituted halo\u20101,2,3\u2010triazoles in biologically relevant molecules.<\/jats:p>","DOI":"10.1002\/cbic.202400150","type":"journal-article","created":{"date-parts":[[2024,3,30]],"date-time":"2024-03-30T06:53:50Z","timestamp":1711781630000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":19,"title":["Halo\u20101,2,3\u2010triazoles: Valuable Compounds to Access Biologically Relevant Molecules"],"prefix":"10.1002","volume":"25","author":[{"given":"Dylan","family":"Coelho","sequence":"first","affiliation":[{"name":"Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques Universit\u00e9 Paris Cit\u00e9, CNRS  F-75006 Paris France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yoann","family":"Colas","sequence":"additional","affiliation":[{"name":"Laboratoire de Chimie et Biochimie 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