SDS of cas: 847818-74-0In 2016 ,《Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors》 appeared in European Journal of Medicinal Chemistry. The author of the article were Zhan, Wenhu; Xu, Lei; Dong, Xiaowu; Dong, Jun; Yi, Xiao; Ma, Xiaodong; Qiu, Ni; Li, Jia; Yang, Bo; Zhou, Yubo; Hu, Yongzhou. The article conveys some information:
A series of novel pyrazolylfuran carboxamides I (24a-d; X = S, R2 = R3 = H; R1, R4: a, H, 4-F; b, Cl, 4-F; c, Br, 4-F; d, H, 3,4-Cl2; 25a-e, X = O, R3 = H, R1, R2, R4: a, Cl, H, 4-F; b, Br, H, 4-F; c, Br, H, 3,4-Cl2; d, Cl, Cl, 4-F; e, Cl, Cl, 3,4-Cl2; 27a-c, X = NMe, R1, R2, R3, R4: a, Br, H, H, 3,4-Cl2; b, Br, Br, H, 3,4-Cl2; c, Cl, Cl, Cl, 3,4-Cl2) and II (26a-c; R1, R2, R4: a, H, Br, 3,4-Cl2; b, Cl, Br, 3,4-Cl2; c, Br, Br, 3,4-Cl2) were designed, synthesized and biol. evaluated for their Akt1 inhibitory activities, as well as anti-proliferative efficacies against HCT116 and OVCAR-8 cell lines. Most compounds exhibited moderate to excellent Akt1 inhibitory activities, together with favorable cytotoxicities. Further kinase selectivity assay of the most promising compound 25e illustrated that it was also potent against the structurally related AGC kinases, including Akt2, Akt3, ROCK1 and PKA, but was specific over kinases from other subfamilies. In addition, the Western blot anal. indicated that 25e could significantly suppress the phosphorylation level of Akt substrate GSK3β in PC-3 cell. Moreover, 25e demonstrated a concentration-dependent inhibition of phosphorylation of PRAS40 in LNCaP cell, with IC50 value of 30.4 nM. In the experiment, the researchers used many compounds, for example, 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0SDS of cas: 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, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. SDS of cas: 847818-74-0
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics