申请人:——
公开号:US20040043969A1
公开(公告)日:2004-03-04
A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.
发现了一系列多样化的微管蛋白结合剂,这些剂在一般意义上结构特征为半刚性的分子框架,能够保持适当的芳基-芳基,伪π堆积距离以进行微管蛋白的分子识别。在酚或氨基形式下,这些配体可以进一步功能化以制备磷酸酯、磷酸盐、磷酰胺和其他前药,能够表现出选择性靶向和破坏肿瘤细胞血管的能力。