2. Academic Validation
  3. Discovery of EBI-1051: A novel and orally efficacious MEK inhibitor with benzofuran scaffold

Discovery of EBI-1051: A novel and orally efficacious MEK inhibitor with benzofuran scaffold

  • Bioorg Med Chem. 2018 Feb 1;26(3):581-589. doi: 10.1016/j.bmc.2017.12.019.
Biao Lu 1,  Song Huang 2,  Jingsong Cao 3,  Qiyue Hu 2,  Ru Shen 3,  Hong Wan 2,  Dan Wang 2,  Jijun Yuan 2,  Lei Zhang 2,  Jiayin Zhang 3,  Minsheng Zhang 3,  Weikang Tao 2,  Lianshan Zhang 2
Affiliations

Affiliations

  • 1 Shanghai Hengrui Pharmaceutical Co. Ltd., 279 Wenjing Rd, Minhang Hi-tech Zone, Shanghai 200245, China. Electronic address: [email protected].
  • 2 Shanghai Hengrui Pharmaceutical Co. Ltd., 279 Wenjing Rd, Minhang Hi-tech Zone, Shanghai 200245, China.
  • 3 Eternity Bioscience Inc., 6 Cedarbrook Drive, Cranbury, NJ 08512, USA.
PMID: 29317148 DOI: 10.1016/j.bmc.2017.12.019
Abstract

A novel series of benzodihydrofuran derivatives was developed as potent MEK inhibitors through scaffold hopping based on known clinical compounds. Further SAR exploration and optimization led to another benzofuran series with good oral bioavailability in rats. One of the compounds EBI-1051 (28d) demonstrated excellent in vivo efficacy in colo-205 tumor xenograft models in mouse and is suitable for pre-clinical development studies for the treatment of melanoma and MEK associated cancers. Compared to AZD6244, EBI-1051 showed superior potency in some Cancer cell lines such as colon-205, A549 and MDA-MB-231.

Keywords

Benzofuran; Kinase; MEK inhibitors; Scaffold hopping.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-111368
    MEK Inhibitor
    MEK