Cancer is a class of formidable disease with high degree of mortality. Despite much progress in
chemotherapy, the problem of drug resistance has led to the search for newer leads with superior efficacy. 1,2,3-
Triazoles are among a vast number of nitrogen containing heterocycles studied extensively as pharmacologically
important scaffolds. Recently developed copper(I)-catalyzed cycloaddition reaction between organic azides and
terminal alkynes yielding 1,4-disubstituted 1,2,3-triazoles has attracted considerable attention because it allows the
construction of a vast array of 1,2,3-triazoles with significant potential in pharmaceutical chemistry. In this article,
an attempt to summarize the wide range of anticancer agents derived from copper(I)-catalyzed azide alkyne
cycloaddition reported by the authors worldwide, has been made. This review includes articles published from
2010 onwards and summarizes the recent progress on the development of 1,4-disubstituted 1H-1,2,3-triazoles as
novel anticancer chemotypes with high therapeutic indices.
Keywords: 1, 2, 3-triazoles, 1, 4-disubstituted 1H-1, 2, 3-triazoles, click chemistry, anticancer agents, nitrogen, chemtherapy.
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