Preliminary SAR analysis of novel antiproliferative N(6),5'-bis-ureidoadenosine derivatives
Matt A Peterson1, Marcelio Oliveira, Michael A Christiansen
1Department of Chemistry and Biochemistry, Brigham Young University, Provo, UT 84602, United States. matt_peterson@byu.edu
Abstract:
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.
Related Concept Videos
Antiviral Nucleoside Inhibitors
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Antiprotozoal Agents
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
