2. Academic Validation
  3. Design, synthesis and anti-TNBC activity of Azeliragon triazole analogues

Design, synthesis and anti-TNBC activity of Azeliragon triazole analogues

  • Bioorg Med Chem Lett. 2021 Dec 15:54:128444. doi: 10.1016/j.bmcl.2021.128444.
Jizhao Xie 1,  Huanji Xu 2,  Xinduo Wu 2,  Yunfeng Xie 2,  Xiuhong Lu 3,  Lisheng Wang 4
Affiliations

Affiliations

  • 1 Medical College, Guangxi University, Nanning 530004, China; School of Pharmaceutical Science, Guangxi Medical University, Nanning 530021, China.
  • 2 School of Pharmaceutical Science, Guangxi Medical University, Nanning 530021, China.
  • 3 Shanghai Key Laboratory of Molecular Imaging, Shanghai University of Medicine and Health Sciences, Shanghai 201318, China. Electronic address: luxh@sumhs.edu.cn.
  • 4 Medical College, Guangxi University, Nanning 530004, China. Electronic address: lswang@gxu.edu.cn.
PMID: 34763082 DOI: 10.1016/j.bmcl.2021.128444
Abstract

Triple-negative breast Cancer (TNBC) is the most aggressive subtype of breast Cancer. Many studies have shown a significant increase in the marker signal of the receptor for advanced glycation end-products (RAGE) with the malignant progression of tumor growth, metastasis and recurrence of breast Cancer, including TNBC of primary tumors and lymph node metastases. Azeliragon is a RAGE inhibitor and it has been shown to actively inhibit the TNBC cell line, SUM149 (IC50 = 5.292 ± 0.310 μM). In order to develop a new anti-TNBC agent, we designed, synthesized and screened 26 Azeliragon triazole analogues to determine their anti-TNBC activities in vitro. The most active compound was KC-10 with an IC50 value of 0.220 ± 0.034 μM.

Keywords

Azeliragon; RAGE inhibitor; SUM149; Triazole analogue; Triple-negative breast cancer.

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