The successful design and pre-clicked synthesis of a non-toxic and cytosol trackable carboplatin-like near infrared fluorophore conjugate via strain-promoted azide alkyne cycloaddition (SPAAC) is reported. Reaction of cis-[Pt(2-azidopropane-1,3-diamine)(cbdca)] (cbdca = cyclobutane-1,1-dicarboxylato) and a bicyclo[6.1.0]non-4-yne near-infrared (NIR) azadipyrromethene fluorophore gave the corresponding clicked Pt-Fluorophore conjugate. The X-ray crystal structure of cis-[Pt(2-azidopropane-1,3-diamine)(cbdca)] was determined featuring the azide on the bidentate 1,3-diaminopropane ligand. The Pt-fluorophore conjugate is the first example of a Pt conjugate clicked via strain-promoted azide alkyne cycloaddition (SPAAC) where the reactive azide handle is on the amine carrier ligand. The in vitro cytotoxicity and widefield fluorescence imaging of the Pt-Fluorophore conjugate in A2780P and A2780cisR cells are described.

报道了通过应变促进的叠氮化物炔烃环加成反应（SPAAC）成功设计和预点击合成无毒且可追踪细胞质的类卡铂近红外荧光团的方法。的反应顺- [PT（2- azidopropane -1,3-二胺）（CBDCA）]（CBDCA =环丁烷-1,1-二dicarboxylato）和二环[6.1.0]壬-4-炔近红外（NIR ）azadipyrromethene荧光团得到相应的单击的Pt-Fluorophore共轭物。以双齿1,3-二氨基丙烷配体上的叠氮化物为特征，测定了顺式-[Pt（2-叠氮丙烷-1,3-二胺）（cbdca）]的X射线晶体结构。Pt-荧光团缀合物是通过点击的Pt缀合物的第一个例子应变促进的叠氮化物炔烃环加成反应（SPAAC），其中反应性叠氮化物手柄位于胺载体配体上。在体外在A2780P和A2780cisR细胞铂-荧光团共轭的细胞毒性和宽场荧光成像进行说明。