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 | Zendy

Jian Zhou | Zendy; Mairéad Reidy | Zendy; Ciaran O’Reilly | Zendy; Dilip V. Jarikote | Zendy; Arvind Negi | Zendy; Afshin Samali | Zendy; Éva Szegezdi | Zendy; Paul V. Murphy | Zendy

Open Access

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

Author(s) -

Jian Zhou,

Mairéad Reidy,

Ciaran O’Reilly,

Dilip V. Jarikote,

Arvind Negi,

Afshin Samali,

Éva Szegezdi,

Paul V. Murphy

Publication year - 2015

Publication title -

organic letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.94

H-Index - 239

eISSN - 1523-7060

pISSN - 1523-7052

DOI - 10.1021/acs.orglett.5b00404

Subject(s) - chemistry , inducer , reductive amination , apoptosis , amination , stereochemistry , combinatorial chemistry , ring (chemistry) , antagonist , triazole , receptor , biochemistry , organic chemistry , gene , catalysis

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.

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