Fluorescent cytotoxic compounds specific for the cellular polyamine transport system
申请人:Phanstiel, IV Otto
公开号:US08410311B1
公开(公告)日:2013-04-02
Cyano-substituted anthracene containing polyamines were synthesized and shown to be efficient polyamine transporter ligands. Moreover, these compounds (3 and 4) had improved fluorescence properties over previously known anthryl-polyamine conjugates, which facilitated their intracellular trafficking by confocal microscopy. These cytotoxic fluorescent agents may find use as molecular probes which traffic into cells via the polyamine transport system and may also be viable anticancer drugs which are readily quantified in human tissues due to their excellent fluorescence properties: (excitation: λ 405 nm) and emission (420 nm) occurs in the visible light range. The ability to excite and emit in the visible range provides an advantage to these probes as these wavelengths are not toxic to human cells (versus ultraviolet mediated excitations, λ<400 nm) and visible light lasers are less costly to purchase and operate than UV laser sources.
含有氰基取代的蒽含有聚胺基团,已合成并证明是高效的聚胺转运体配体。此外,这些化合物(3和4)具有比先前已知的蒽基聚胺共轭物更好的荧光性能,这有助于它们通过共聚焦显微镜的细胞内转运。这些具有细胞毒性的荧光剂可能被用作分子探针,通过聚胺转运系统进入细胞,也可能是易于在人体组织中定量的有效抗癌药物,因为它们具有出色的荧光性能:(激发波长:λ 405 nm),发射波长在可见光范围内(420 nm)。在可见光范围内激发和发射的能力为这些探针提供了优势,因为这些波长对人体细胞不具有毒性(与紫外线介导的激发相比,λ<400 nm),而可见光激光器的购买和运行成本较紫外激光源更低。