UMR 176 CNRS/Institut Curie, Institut Curie, Bât 110, University Paris-Sud, F-91405 Orsay, France.
J Org Chem. 2011 Apr 1;76(7):2010-28. doi: 10.1021/jo102185d. Epub 2011 Mar 1.
This paper describes the conception, synthesis, and characterization of new tetrapyrrolic chromophores bearing glycodendrimeric moieties inducing a potential increase of tumor targeting by a cluster effect. Two families of monoglycodendrimeric photosensitizers bearing three glycosyl units were designed, prepared with an acceptable overall efficiency and characterized by NMR, UV-visible, and fluorescence spectroscopies. The polarity and log P were evaluated by HPLC and the stir-flask method, respectively. The in vitro photoefficiency against two human tumor cell lines was assessed. The presence of the glycodendrimeric group does not appear to increase the tumor in vitro targeting.
本文描述了新型四吡咯生色团的概念、合成和表征，这些生色团带有糖树枝状大分子部分，通过簇效诱导潜在的肿瘤靶向性增加。设计了两种带有三个糖基单元的单糖树枝状大分子光敏剂，以可接受的总效率制备，并通过 NMR、UV-可见和荧光光谱进行了表征。通过 HPLC 和搅拌瓶法分别评估了极性和 log P。评估了对两种人肿瘤细胞系的体外光效。糖树枝状大分子基团的存在似乎不会增加体外肿瘤靶向性。
