2. Academic Validation
  3. The discovery of novel N-(2-pyrimidinylamino) benzamide derivatives as potent hedgehog signaling pathway inhibitors

The discovery of novel N-(2-pyrimidinylamino) benzamide derivatives as potent hedgehog signaling pathway inhibitors

  • Bioorg Med Chem Lett. 2013 Dec 15;23(24):6777-83. doi: 10.1016/j.bmcl.2013.10.022.
Minhang Xin 1,  Jun Wen,  Feng Tang,  Chongxing Tu,  Han Shen,  Xinge Zhao
Affiliations

Affiliation

  • 1 Jiangsu Simcere Pharmaceutical Co. Ltd, Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research, No. 699-18, Xuan Wu District, Nanjing 210042, PR China. Electronic address: xmhcpu@163.com.
PMID: 24176396 DOI: 10.1016/j.bmcl.2013.10.022
Abstract

Hedgehog signaling pathway inhibitors are emerging as new therapeutic intervention against Cancer. A novel series of N-(2-pyrimidinylamino) benzamide derivatives as Hedgehog signaling pathway inhibitors were designed and synthesized. Most compounds presented significant inhibitory effect on Hedgehog signaling pathway, among which 21 compounds exhibited more potent than vismodegib. Furthermore, compound 6a showed moderate pharmacokinetic properties in vivo, representing a promising lead compound for further exploration.

Keywords

Hedgehog signaling; Hedgehog signaling pathway inhibitors; Lead compound; Synthesize.

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