Medical College, Guangxi University, Nanning 530004, China; School of Pharmaceutical Science, Guangxi Medical University, Nanning 530021, China.
School of Pharmaceutical Science, Guangxi Medical University, Nanning 530021, China.
Bioorg Med Chem Lett. 2021 Dec 15;54:128444. doi: 10.1016/j.bmcl.2021.128444. Epub 2021 Nov 9.
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 (IC = 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 IC value of 0.220 ± 0.034 μM.
三阴性乳腺癌（TNBC）是乳腺癌中最具侵袭性的亚型。许多研究表明，晚期糖基化终产物受体（RAGE）的标志物信号随着肿瘤生长、转移和乳腺癌复发的恶性进展而显著增加，包括原发性肿瘤和淋巴结转移的 TNBC。Azeliragon 是一种 RAGE 抑制剂，已被证明可积极抑制 TNBC 细胞系 SUM149（IC = 5.292 ± 0.310 μM）。为了开发一种新的抗 TNBC 药物，我们设计、合成并筛选了 26 种 Azeliragon 三唑类似物，以确定它们在体外的抗 TNBC 活性。最活跃的化合物是 KC-10，其 IC 值为 0.220 ± 0.034 μM。
