咪唑并[1,2-b]吡唑-7-甲酰胺的合成、细胞毒性表征和构效关系研究。
Synthesis, cytotoxic characterization, and SAR study of imidazo[1,2-b]pyrazole-7-carboxamides.
机构信息
AVIDIN Ltd., Szeged, Hungary.
Department of Organic Chemistry, University of Szeged, Szeged, Hungary.
出版信息
Arch Pharm (Weinheim). 2018 Jul;351(7):e1800062. doi: 10.1002/ardp.201800062. Epub 2018 Jun 10.
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 analogues exhibited sub-micromolar activities, from which compound 63 exerted the most significant potency with a remarkable HL-60 sensitivity (IC = 0.183 μM).
研究了新型咪唑并[1,2-b]吡唑-7-甲酰胺的合成及体外细胞毒性特征。通过对 MCF-7 人乳腺癌、4T1 乳腺和 HL-60 人早幼粒细胞白血病癌细胞系的 2D 和 3D 培养进行的从头至先导优化，构建了一个 67 成员的文库，并确定了结构-活性关系 (SAR)。七种合成的类似物表现出亚微摩尔的活性，其中化合物 63 表现出最强的活性，对 HL-60 具有显著的敏感性 (IC = 0.183 μM)。
Zotero 插件