The [1,4]benzodiazepine is an important class of heterocyclic compounds and clinically used for many ailments
in humans. The [1,4]benzodiazepine has unique structure that mimics the peptide linkage. This interesting observation
completely shifted the interest of medicinal chemist for [1,4]benzodiazepine from CNS acting drugs to anticancer agents.
During last few decades, a large number of reports have appeared in the literature highlighting the anticancer activity of
[1,4]benzodiazepines. Here, in this article, we have discussed the brief synthesis, origin of [1,4]benzodiazepines as
anticancer agent, their mechanism of action and latest developments in this field. We have compiled the most important
literature reports from last few decades till date.
Keywords: Anticancer, [1, 4]Benzodiazepines, DNA intercalating agents, Pyrrolo[1, 4]benzodiazepine, Antiarrhythmic agents,
2-Azidobenzoylchloride, Histone deacetylase inhibitors, Columbic interactions.
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