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Tryptanthrin and Its Derivatives in Drug Discovery: Synthetic Insights

Marta Piñeiro, Pedro Brandão, Anthony J. Burke

2022Synthesis14 citationsDOIOpen Access PDF

Abstract

Abstract Tryptanthrin is a golden-yellow, naturally occurring alkaloid that can be obtained from multiple sources and through different synthetic methodologies. This tetracyclic compound displays several relevant biological activities. The potential of this tetracyclic alkaloid has been widely explored, and several researchers have focused their attention on expanding the variety of tryptanthrin derivatives by using a range of synthetic strategies. In this short review, we aim to address recent developments in the synthesis of the tryptanthrin core, as well as the development of new strategies employed by synthetic organic chemists to obtain novel tryptanthrin derivatives with potential biological activity, using different tools from the chemists’ toolbox, such as photocatalysis, solvent-free approaches, and multicomponent reactions.

Topics & Concepts

ChemistryDrug discoveryCombinatorial chemistryToolboxAlkaloidOrganic chemistryNanotechnologyBiochemistryComputer scienceMaterials scienceProgramming languageQuinazolinone synthesis and applicationsPhenothiazines and Benzothiazines Synthesis and ActivitiesSynthesis and Biological Evaluation