Synthesis and Investigation of S-Substituted 2-Mercaptobenzoimidazoles as Inhibitors of Hedgehog Signaling. Gräßle, S., Susanto, S., Sievers, S., Tavsan, E., Nieger, M., Jung, N., & Bräse, S. ACS Medicinal Chemistry Letters, 8:931-935, American Chemical Society, 9, 2017.
doi  abstract   bibtex   
Due to the arising resistance of common drugs targeting the Hedgehog signaling pathway, the identification of new compound classes with inhibitory effect is urgently needed. We were able to identify S-alkylated 2-mercaptobenzoimidazoles as a new compound class that exhibits Hedgehog signaling activity in a low micromolar range. The scope of the 2-mercaptobenzoimidazole motif has been investigated by the syntheses of diverse derivatives, revealing that the elongation of the linker unit and the exchange of particular substitution patterns are tolerable with respect to the activity of the compound class.
@article{,
   abstract = {Due to the arising resistance of common drugs targeting the Hedgehog signaling pathway, the identification of new compound classes with inhibitory effect is urgently needed. We were able to identify S-alkylated 2-mercaptobenzoimidazoles as a new compound class that exhibits Hedgehog signaling activity in a low micromolar range. The scope of the 2-mercaptobenzoimidazole motif has been investigated by the syntheses of diverse derivatives, revealing that the elongation of the linker unit and the exchange of particular substitution patterns are tolerable with respect to the activity of the compound class.},
   author = {Simone Gräßle and Steven Susanto and Sonja Sievers and Emel Tavsan and Martin Nieger and Nicole Jung and Stefan Bräse},
   doi = {10.1021/acsmedchemlett.7b00100},
   issn = {19485875},
   issue = {9},
   journal = {ACS Medicinal Chemistry Letters},
   keywords = {2-mercaptobenzoimidazoles,Hedgehog signaling,cancer,small molecules},
   month = {9},
   pages = {931-935},
   publisher = {American Chemical Society},
   title = {Synthesis and Investigation of S-Substituted 2-Mercaptobenzoimidazoles as Inhibitors of Hedgehog Signaling},
   volume = {8},
   year = {2017},
}

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