Polyethylene glycol conjugates of methotrexate varying in their molecular weight from MW 750 to MW 40000: synthesis, characterization, and structure-activity relationships in vitro and in vivo.

@article{Riebeseel2002PolyethyleneGC,
  title={Polyethylene glycol conjugates of methotrexate varying in their molecular weight from MW 750 to MW 40000: synthesis, characterization, and structure-activity relationships in vitro and in vivo.},
  author={Katja Riebeseel and Elfi Biedermann and R. Loeser and Norbert Breiter and Ralf Hanselmann and R Rolf M{\"u}lhaupt and Clemens Unger and Felix Kratz},
  journal={Bioconjugate chemistry},
  year={2002},
  volume={13 4},
  pages={773-85}
}
Poly(ethylene glycol)s (PEGs) are potential drug carriers for improving the therapeutic index of anticancer agents. In this work, the anticancer drug methotrexate (MTX) was activated with N,N'-dicyclohexylcarbodiimide (DCC) and coupled to amino group bearing PEGs of MW 750, 2000, 5000, 10 000, 20,000, and 40,000. First, the activation process of MTX with DCC in the presence and absence of N-hydroxysuccinimide was analyzed through HPLC. Preincubation of methotrexate with DCC alone at 0 degrees C… CONTINUE READING