Decorated macrocycles via ring-closing double-reductive amination. Identification of an apoptosis inducer of leukemic cells that at least partially antagonizes a 5-HT2 receptor
Jarikote, Dilip V.
Murphy, Paul V.
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Zhou, J,Reidy, M,O'Reilly, C,Jarikote, DV,Negi, A,Samali, A,Szegezdi, E,Murphy, PV (2015) 'Decorated Macrocycles via Ring-Closing Double-Reductive Amination. Identification of an Apoptosis Inducer of Leukemic Cells That at Least Partially Antagonizes a 5-HT2 Receptor'. Organic Letters, 17 :1672-1675.
A build-couple-pair strategy, including double-reductive amination macrocyclization, has been used to generate decorated macrocycles (eannaphanes) with an embedded triazole and monosaccharide. Biological screening led to the identification of an inducer of apoptosis in leukemic cells, which acts at least partially as a 5-HT2 antagonist.