Synthesis and evaluation of 4-(2-pyrimidinylamino) benzamides inhibitors of hedgehog signaling pathway.

Bioorg Med Chem Lett

Jiangsu Simcere Pharmaceutical Co. Ltd., Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research, No 699-18, Xuan Wu District, Nanjing 210042, P.R. China.

Published: February 2014

AI Article Synopsis

  • A new series of inhibitors targeting the hedgehog signaling pathway has been created using a specific chemical structure called 4-(2-pyrimidinylamino) benzamides.
  • The process of making these compounds and examining their structure-activity relationships (SAR) is detailed in the study.
  • Among them, compound 3c has been identified as a strong and easy-to-take option with better physical and drug-like properties.

Article Abstract

A novel series of hedgehog signaling pathway inhibitors has been designed based on the 4-(2-pyrimidinylamino) benzamides scaffold. The synthesis and SAR of these compounds are described. Optimization leads to the identification of compound 3c, a potent and orally available agent with improved physicochemical and pharmacokinetic properties.

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Source
http://dx.doi.org/10.1016/j.bmcl.2013.12.050DOI Listing

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