Retraction of “Design and Synthesis of Novel Cyclic Amine

Feb 23, 2017 - Joncour, Desroy, Housseman, Bock, Bienvenu, Cherel, Labeguere, Peixoto, Annoot, Lepissier, Heiermann, Hengeveld, Pilzak, Monjardet, Wak...
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Retraction pubs.acs.org/jmc

Retraction of “Design and Synthesis of Novel Cyclic Amine Benzimidazoles for the Treatment of Pancreatic Cancer” Vibha Pathak, Corinne E. Augelli-Szafran,* Han-Xun Wei, Yonghe Li, Patsy G. Oliver, Wenyan Lu, Donald J. Buchsbaum, and Mark J. Suto S Supporting Information *

The authors retract the article “Design and Synthesis of Novel Cyclic Amine Benzimidazoles for the Treatment of Pancreatic Cancer”, J. Med. Chem., 2017, DOI: 10.1021/acs.jmedchem.6b01417, on the basis that aspects of the interpretation of the experimental data were found to be incorrect. Postpublication analysis of results was prompted by a publication (Chem. Biol. 2012, 19, 1060−1072 DOI: 10.1016/j.chembiol.2012.07.015) that reported that some compound classes, such as benzimidazoles, inhibit luciferase activity. Since the Wnt assay, which was employed to generate the IC50 values in Tables 1−4 of the J. Med. Chem. manuscript, used luciferase as a reporter, we tested if the compounds reported in our published article inhibited Wnt-mediated transcriptional activation of luciferase, rather than inhibiting the enzymatic activity of the reporter enzyme. We therefore evaluated representative compounds reported in the manuscript in a HEK cell-line in which luciferase is produced by a promoter that is not driven by Wnt. The data showed that most of the tested compounds were active in this assay and had similar potencies to those obtained in our Wnt assay. We conclude that these representative compounds are inhibiting luciferase enzyme activity rather than Wnt signaling. Accordingly, the SAR conclusions reported in our J. Med. Chem. manuscript are incorrect. The original article was published as a Just Accepted manuscript on February 23, 2017, and retracted on September 14, 2017. The PDF content of the original publication accompanies this Retraction as Supporting Information.



ASSOCIATED CONTENT

S Supporting Information *

The Supporting Information is available free of charge on the ACS Publications website at DOI: 10.1021/acs.jmedchem.6b01417 The original published work has been appended as Supporting Information (PDF)

Received: September 25, 2016 Published: February 23, 2017 © 2017 American Chemical Society

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DOI: 10.1021/acs.jmedchem.6b01417 J. Med. Chem. 2017, 60, 7615−7615