Tryptanthrin: Synthetic advances and therapeutic horizons of a privileged scaffold
Nilufar Yasmin Mostafa1, Debashis Dutta1, Bandana Das1
1Department of Pharmaceutical Sciences, Sushruta School of Medical and Paramedical Sciences, Assam University, Silchar, Assam, 788011, India.
Abstract:
Tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione) is a privileged scaffold distinguished by its rigid tetracyclic framework and exceptional pharmacological breadth. This review critically analyzes advancements in the chemistry and biology of tryptanthrin, prioritizing post-2020 literature. We elucidate its natural occurrence and innovative synthetic strategies, spanning from classical condensation to sustainable photochemical and electrochemical methods. The review examines the therapeutic landscape of tryptanthrin chemotypes, highlighting anticancer efficacy via kinase and topoisomerase modulation. Furthermore, we explore emerging utility against multidrug-resistant bacteria, SARS-CoV-2, and neurodegenerative conditions. By integrating structure-activity relationship data with mechanistic insights, this work underscores tryptanthrin as a versatile pharmacophore for the rational design of next-generation therapeutics.
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