2. Academic Validation
  3. Design, synthesis and biological evaluation of quinazoline SOS1 inhibitors

Design, synthesis and biological evaluation of quinazoline SOS1 inhibitors

  • Bioorg Med Chem Lett. 2023 May 15:88:129265. doi: 10.1016/j.bmcl.2023.129265.
Hongyu Jiang 1,  Yiqing Fan 1,  Xia Wang 1,  Jie Wang 1,  Haifan Yang 1,  Weizheng Fan 2,  Chunlei Tang 3
Affiliations

Affiliations

  • 1 School of Life Sciences and Health Engineering, Jiangnan University, Wuxi, China.
  • 2 School of Life Sciences and Health Engineering, Jiangnan University, Wuxi, China. Electronic address: wzfan@jiangnan.edu.cn.
  • 3 School of Life Sciences and Health Engineering, Jiangnan University, Wuxi, China. Electronic address: tangcl@jiangnan.edu.cn.
PMID: 37011767 DOI: 10.1016/j.bmcl.2023.129265
Abstract

Son of sevenless 1 (SOS1) is a vital guanine nucleotide exchange factor (GEFs) that activates rat sarcoma (Ras) protein in cells. SOS1 inhibitors can effectively inhibit the expression of downstream signaling pathways by blocking the interaction between SOS1 and Ras protein. Here, we designed and synthesized a series of quinazoline-based compounds, and conducted subsequent evaluations of their biological activities. Among them, the comparable compounds I-2 (IC50 = 20 nM, against SOS1) I-5 (IC50 = 18 nM, against SOS1) and I-10 (IC50 = 8.5 nM, against SOS1) have kinase activity equivalent to BAY-293 (IC50 = 6.6 nM, against SOS1), and I-10 also has cell activity equivalent to BAY-293, providing a theoretical reference for subsequent related researches on SOS1 inhibitors.

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