Inclusion Complexes of 2-Chloroethylnitrososulfamides (CENS) in Natural and Modified β- Cyclodextrins

A series of nine inclusion complexes have been prepared in the solid state between three different 2- chloroethylnitrososulfamides (CENS) and three different cyclodextrins (β-cyclodextrin, methyl-β-cyclodextrin and (2- hydroxylpropyl)-β-cyclodextrin). The formation of inclusion complexes with a 1/1 stoichiometry has been confirmed. NMR studies showed that the CENS moiety is encapsulated in CDs cavities in a tilted equatorial orientation. Since biological evaluation showed that the cyclodextrins have only a slight effect on the activity of the drugs toward two cancer cell lines, the possibility exists that the complexes may find pharmaceutical use by improving the drugs' in vivo bioavailability and stability.