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A new scaffold of topoisomerase I inhibitors: Design, synthesis and biological evaluation.
European Journal of Medicinal Chemistry 2016 November 30
The synthesis of a new hexacyclic system was realized starting from tryptamines and exploiting as a key step a sequential Pd-catalyzed N-arylation/acylation reaction. Having topoisomerases as biological target and the campthotecins class as benchmark, the new scaffold was decorated with substituents having different polarity and tested as Topoisomerase I inhibitors.
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