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Synthesis and Investigation of -Substituted 2-Mercaptobenzoimidazoles as Inhibitors of Hedgehog Signaling. | LitMetric

Synthesis and Investigation of -Substituted 2-Mercaptobenzoimidazoles as Inhibitors of Hedgehog Signaling.

ACS Med Chem Lett

Institute of Toxicology and Genetics, Karlsruhe Institute of Technology, Campus North, Hermann-von-Helmholtz-Platz 1, 76344 Eggenstein-Leopoldshafen, Germany.

Published: September 2017

AI Article Synopsis

  • There is a growing resistance to common drugs that target the Hedgehog signaling pathway, creating a need for new treatment options.
  • Researchers discovered a new class of compounds called -alkylated 2-mercaptobenzoimidazoles that effectively inhibit Hedgehog signaling at low micromolar concentrations.
  • The study explored various derivatives of 2-mercaptobenzoimidazole, showing that modifying the linker and substituent patterns still maintains their activity.

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 -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.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5601384PMC
http://dx.doi.org/10.1021/acsmedchemlett.7b00100DOI Listing

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