基于球体的细胞血管生成试验中钛茂化合物的分析。
Analyses of Titanocenes in the spheroid-based cellular angiogenesis assay.
作者信息
Weber Holger, Claffey James, Hogan Megan, Pampillón Clara, Tacke Matthias
机构信息
ProQinase GmbH Freiburg, Breisacher Str. 117, D-79106 Freiburg, Germany.
出版信息
Toxicol In Vitro. 2008 Mar;22(2):531-4. doi: 10.1016/j.tiv.2007.09.014. Epub 2007 Sep 29.
Titanocene dichloride and two of its derivatives (Titanocene Y and C) were tested on human umbilical vein endothelial cells (HUVEC) sprouting in a spheroid-based cellular angiogenesis assay in order to determine IC50 values of inhibition. Titanocene dichloride and Titanocene Y inhibited HUVEC sprouting in this angiogenesis assay with IC50 values of 19 microM and 4.9 microM, while Titanocene C surprisingly showed no inhibition. This classifies Titanocene dichloride as a purely anti-angiogenic anticancer drug and Titanocene C as a purely cytotoxic anticancer drug. On the other hand, Titanocene Y combines both favourable anticancer activities and seems to be the drug candidate of choice for further optimisation.
二氯二茂钛及其两种衍生物（二茂钛Y和二茂钛C）在基于球体的细胞血管生成试验中对人脐静脉内皮细胞（HUVEC）的发芽进行了测试，以确定抑制的IC50值。在该血管生成试验中，二氯二茂钛和二茂钛Y抑制HUVEC发芽，IC50值分别为19 microM和4.9 microM，而二茂钛C出人意料地未显示出抑制作用。这将二氯二茂钛归类为纯粹的抗血管生成抗癌药物，将二茂钛C归类为纯粹的细胞毒性抗癌药物。另一方面，二茂钛Y兼具两种良好的抗癌活性，似乎是进一步优化的首选候选药物。
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