ArticleBioorganic & medicinal chemistry letters2021
Design and synthesis of C-aryl angular luotonins via a one-pot aza-Nazarov-Friedlander sequence and their Topo-I inhibition studies along with C-aryl vasicinones and luotonins.
Article in Bioorganic & medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- Brønsted-Acid-Promoted Diaza-Nazarov Cyclization to Access Tetrasubstituted Pyrazoles.Organic letters · 2025Article
- Quinazolines [Molecules (Basel, Switzerland) · 2025Review
- Recent Advances in the Research on Luotonins A, B, and E.Molecules (Basel, Switzerland) · 2024Review
- Diversity oriented total synthesis (DOTS) of pyridoquinazolinone alkaloids and their analogues.Tetrahedron chem · 2024Article
- Catalytic aza-Nazarov cyclization reactions to access α-methylene-γ-lactam heterocycles.Beilstein journal of organic chemistry · 2023Article
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Abstract
A facile one-pot synthesis of C-ring substituted angular luotonins has been realized via a methanesulfonic acid mediated aza-Nazarov-Friedlander condensation sequence on quinazolinonyl enones. Topoisomerase I (topo-I) inhibition studies revealed that the angular luotonin library (7a-7l) and their regioisomeric analogs (linear luotonins, 8a-8l) are weak negative modulators, compared to camptothecin. These results would fare well for the design of topo-I-inert luotonins for non-oncological applications such as anti-fungal and insecticide lead developments. Surprisingly, the tricyclic vasicinones (9h, 9i, and 9j) showed better topo-I inhibition compared to pentacyclic C-aryl luotonins providing a novel pharmacophore for further explorations.
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