In vitro activity of resorcinarene–chlorambucil conjugates for therapy in human chronic myelogenous leukemia cells

Abstract

A possible way of improving the activity and selectivity profile of antitumor agents is to design drug carrier systems employing soluble macromolecules. Thus, four resorcinarene-PAMAM-dendrimer conjugates of chlorambucil with different groups in the lower part of the macrocycle and different length dendritic arms showed a good stability of the chemical link between drug and spacer. Evaluation of the cytotoxicity of the resorcinarene-PAMAM-dendrimer–chlorambucil conjugate employing a sulforhodamine B (SRB) assay in K-562 (human chronic myelogenous leukemia cells) demonstrated that the conjugate was more potent as an antiproliferative agent than chlorambucil.

Keywords:

• Leukemia cancer
• chlorambucil
• conjugates
• dendrimers
• resorcinarene

Acknowledgements

The authors thank Rios O. H., Velasco L., Huerta S. E., Patiño M. M. R., Peña Gonzalez M. A., and Antonio Nieto Camacho for technical assistance.

Disclosure statement

The authors confirm that this article content has no conflict of interest.

Additional information

Funding

This work was supported by DGAPA [IN101117] grants. EMK was supported by a postdoctoral fellowship from DGAPA-UNAM.