Synthesis and characterisation of 5-acyl-6,7-dihydrothieno[3,2-c]pyridine inhibitors of Hedgehog acyltransferase

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• 作者：Thomas Lanyon-Hogg^a ; Naoko Masumoto^a ; George Bodakh^a ; Antonio D. Konitsiotis^b ; ¹ ; Emmanuelle Thinon^a ; ² ; Ursula R. Rodgers^b ; Raymond J. Owens^c ; Anthony I. Magee^b ; ^{t.magee@imperial.ac.uk" class="auth_mail" title="E-mail the corresponding author} ; Edward W. Tate^a ; ^{e.tate@imperial.ac.uk" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Synthesis ; Inhibitors ; Hedgehog acyltransferase ; Conformation
• 刊名：Data in Brief
• 出版年：2016
• 出版时间：June 2016
• 年：2016
• 卷：7
• 期：Complete
• 页码：257-281
• 全文大小：4333 K

文摘

In this data article we describe synthetic and characterisation data for four members of the 5-acyl-6,7-dihydrothieno[3,2-c]pyridine (termed “RU-SKI”) class of inhibitors of Hedgehog acyltransferase, including associated NMR spectra for final compounds. RU-SKI compounds were selected for synthesis based on their published high potencies against the enzyme target. RU-SKI 41 (ass="boldFont">9a), RU-SKI 43 (ass="boldFont">9b), RU-SKI 101 (ass="boldFont">9c), and RU-SKI 201 (ass="boldFont">9d) were profiled for activity in the related article “Click chemistry armed enzyme linked immunosorbent assay to measure palmitoylation by Hedgehog acyltransferase” (Lanyon-Hogg et al., 2015) an id="bbib1">[1]a>an>. ¹H NMR spectral data indicate different amide conformational ratios between the RU-SKI inhibitors, as has been observed in other 5-acyl-6,7-dihydrothieno[3,2-c]pyridines. The synthetic and characterisation data supplied in the current article provide validated access to the class of RU-SKI inhibitors.