Xie, Jizhao; Xu, Huanji; Wu, Xinduo; Xie, Yunfeng; Lu, Xiuhong; Wang, Lisheng published their research in Bioorganic & Medicinal Chemistry Letters in 2021. The article was titled 《Design, synthesis and anti-TNBC activity of Azeliragon triazole analogues》.Application of 847818-74-0 The article contains the following contents:
Triple-neg. 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 analogs to determine their anti-TNBC activities in vitro. The most active compound was KC-10 (3-(4-(5-butyl-1-(4′-chloro-[1,1′-biphenyl]-4-yl)-1H-1,2,4-triazol-3-yl)phenoxy)-N, N-diethylpropan-1-amine) with an IC50 value of 0.220 ± 0.034 μM. The experimental part of the paper was very detailed, including the reaction process of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Application of 847818-74-0)
1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. Application of 847818-74-0
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics