Preliminary SAR analysis of novel antiproliferative N(6),5'-bis-ureidoadenosine derivatives.

A preliminary library of novel N(6),5'-bis-ureidoadenosine analogs and related derivatives was prepared and tested for activity against the NCI 60 panel of human cancers. A 2'-O-TBS group was found to be necessary, but not sufficient, for optimal antiproliferative activity. Neither the N(6)- nor 5'-ureido substituents were sufficient to achieve significant antiproliferative effects when present in the absence of the other. The 2'-O-TBS, and N(6),5'-bis-ureido substitution patterns were found to be necessary for optimal antiproliferative activity.