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

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

  • Bioorg Med Chem Lett. 2014 Feb 1;24(3):983-8. doi: 10.1016/j.bmcl.2013.12.050.
Minhang Xin 1,  Jun Wen 2,  Feng Tang 2,  Chongxing Tu 2,  Wei Huang 2,  Han Shen 2,  Xinge Zhao 2,  Lingfei Cheng 2,  Mengyu Wang 2,  Liandi Zhang 2
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Health Science Center, Xi'an Jiaotong University, No. 76, Yanta West Road, Xi'an 710061, P.R. China; 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. Electronic address: xmhcpu@163.com.
  • 2 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.
PMID: 24405704 DOI: 10.1016/j.bmcl.2013.12.050
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.

Keywords

Hedgehog signaling pathway; Inhibitors; Pharmacokinetic properties; SAR.

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