Many metal chelators have polar or charged functional groups, which render them difficult to transport across a cell membrane. Polyamine-metal chelator conjugates of the invention are compounds comprising a first moiety which is a metal chelator and a second moiety which is a polyamine, where the polyamine moiety includes three or more nitrogen atoms which are capable of being positively charged at physiological pH. A spermine-L1 conjugate has been shown to accumulate in L1210 cells several hundred fold more than the unconjugated L1 chelator.
许多
金属
螯合剂具有极性或带电的功能基团,这使得它们难以跨越细胞膜。本发明的
多胺-
金属
螯合剂共轭物是化合物,包括第一部分是
金属
螯合剂,第二部分是
多胺,其中
多胺部分包括三个或更多的氮原子,在生理pH下能够呈正电荷。已经证明
精胺-L1共轭物在L1210细胞中的积累比未共轭的L1
螯合剂高出数百倍。