Synthesis, cytotoxic characterization, and SAR study of imidazo[1,2-<i>b</i>
]pyrazole-7-carboxamides
作者:András Demjén、Róbert Alföldi、Anikó Angyal、Márió Gyuris、László Hackler、Gábor J. Szebeni、János Wölfling、László G. Puskás、Iván Kanizsai
DOI:10.1002/ardp.201800062
日期:2018.7
The synthesis and in vitro cytotoxic characteristics of new imidazo[1,2‐b]pyrazole‐7‐carboxamides were investigated. Following a hit‐to‐lead optimization exploiting 2D and 3D cultures of MCF‐7 human breast, 4T1 mammary gland, and HL‐60 human promyelocytic leukemia cancer cell lines, a 67‐membered library was constructed and the structure–activity relationship (SAR) was determined. Seven synthesized
研究了新型咪唑并[1,2-b]吡唑-7-甲酰胺的合成和体外细胞毒特性。在利用 MCF-7 人乳腺、4T1 乳腺和 HL-60 人早幼粒细胞白血病癌细胞系的 2D 和 3D 培养物进行先导优化后,构建了一个 67 元文库,并构建了构效关系(SAR ) 确定。七个合成的类似物表现出亚微摩尔活性,其中化合物 63 发挥最显着的效力,具有显着的 HL-60 敏感性(IC50 = 0.183 μM)。