2. Academic Validation
  3. Structure-based design and synthesis of bicyclic fused-pyridines as MEK inhibitors

Structure-based design and synthesis of bicyclic fused-pyridines as MEK inhibitors

  • Bioorg Med Chem Lett. 2014 Jun 1;24(11):2555-9. doi: 10.1016/j.bmcl.2014.03.086.
Hejun Lu 1,  Wangyang Tu 2,  Hongbo Fei 2,  Guoji Xu 2,  Qiyue Hu 2,  Lei Zhang 2,  Bing Lin 2,  Jijun Yuan 2,  Junzhao Yin 2,  Aishen Gong 2,  Mimi Wan 2,  Dan Wang 2,  Xiaoyan Zhu 2,  Jun Feng 2,  Qian Wang 2,  Piaoyang Sun 2
Affiliations

Affiliations

  • 1 Shanghai Hengrui Pharmaceutical Co., Ltd, 279 Wenjing Rd., Minhang District, Shanghai 200245, China. Electronic address: lvhj@shhrp.com.
  • 2 Shanghai Hengrui Pharmaceutical Co., Ltd, 279 Wenjing Rd., Minhang District, Shanghai 200245, China.
PMID: 24755426 DOI: 10.1016/j.bmcl.2014.03.086
Abstract

The MAPK pathway is identified as one of the most important pathways involved in cell proliferation and differentiation. A key kinase in the pathway, the Mitogen-activated protein kinase kinase (MEK) is recognized as a promising target for antitumor drugs. Structure-based design and optimization of known MEK inhibitors resulted in identification of compound 10a as a potent non-ATP competitive MEK Inhibitor in both in vitro and in vivo tests.

Keywords

Bicyclic; Cancer; Fused-pyridine; MEK; SBDD.

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