Palladium-catalyzed synthesis and nucleotide pyrophosphatase inhibition of benzo[4,5]furo[3,2-b]indoles
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Date
2019
Volume
15
Issue
Journal
Beilstein journal of organic chemistry
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Frankfurt, Main : Beilstein-Institut zur Förderung der Chemischen Wissenschaften
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Abstract
A two-step palladium-catalyzed procedure based on Suzuki–Miyaura cross coupling, followed by a double Buchwald–Hartwig reaction, allows for the synthesis of pharmaceutically relevant benzo[4,5]furo[3,2-b]indoles in moderate to very good yield. The synthesized compounds have been analyzed with regard to their inhibitory activity (IC50) of nucleotide pyrophosphatases h-NPP1 and h-NPP3. The activity lies in the nanomolar range. The results were rationalized based on docking studies. © 2019 Do et al.
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Do, H. H., Ullah, S., Villinger, A., Lecka, J., Sévigny, J., Ehlers, P., et al. (2019). Palladium-catalyzed synthesis and nucleotide pyrophosphatase inhibition of benzo[4,5]furo[3,2-b]indoles (Frankfurt, Main : Beilstein-Institut zur Förderung der Chemischen Wissenschaften). Frankfurt, Main : Beilstein-Institut zur Förderung der Chemischen Wissenschaften. https://doi.org//10.3762/bjoc.15.276
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CC BY 4.0 Unported