Synthesis and antiproliferative activity of some 3-(pyrid-2-yl)-pyrazolines
Synthesis and antiproliferative activity of some 3-(pyrid-2-yl)-pyrazolines
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DOI：
10.1039/c3md00077j
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发表时间：
2013-06-01
期刊：
影响因子：
--
通讯作者：
Caggiano, Lorenzo
中科院分区：
文献类型：
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作者：
Ciupa, Alexander;De Bank, Paul A.;Caggiano, Lorenzo
报道了11种3-（吡啶-2-基）-吡唑啉的合成及其在两种癌细胞中的抗增殖活性。在NCI 60人肿瘤细胞系中筛选到先导化合物8i，获得了其亚微摩尔活性的x射线晶体形貌。细胞周期分析，体外微管蛋白测定和共聚焦显微镜也有报道，表明先导化合物破坏微管的形成。
The synthesis and antiproliferative activity of eleven 3-(pyrid-2-yl)-pyrazolines in two cancer cell lines are reported. X-ray crystallography was obtained of the lead compound 8i which was screened in the NCI 60 human tumour cell line and displayed sub-micromolar activity. Cell cycle analysis, in vitro tubulin assay and confocal microscopy are also reported and suggest that the lead compound disrupts microtubule formation.