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Back Cover: A Tryptoline Ring‐Distortion Strategy Leads to Complex and Diverse Biologically Active Molecules from the Indole Alkaloid Yohimbine (Chem. Eur. J. 18/2017)
Author(s) -
Paciaroni Nicholas G.,
Ratnayake Ranjala,
Matthews James H.,
Norwood Verrill M.,
Arnold Austin C.,
Dang Long H.,
Luesch Hendrik,
Huigens Robert W.
Publication year - 2017
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201605731
Subject(s) - indole test , yohimbine , small molecule , ring (chemistry) , chemistry , stereochemistry , molecule , indole alkaloid , biological activity , combinatorial chemistry , alkaloid , in vitro , biochemistry , organic chemistry , receptor , antagonist
A tryptoline‐based ring distortion strategy enabled rapid access to an array of complex and diverse molecular scaffolds synthesized from the indole alkaloid, yohimbine. During these investigations, 70 complex and diverse small molecules were synthesized and subjected to a panel phenotype screen. These efforts led to the identification of several biologically active hit compounds, including one compound that demonstrates HIF‐dependent antiproliferative activity in HCT116 (colorectal cancer) cells. More information can be found in the Full Paper by R. W. Huigens III et al. on page 4327 ff.