CNS Cancer Cell Line Cytotoxicity Profiles of Some 2, 6, 9-Substituted Purines: A Comparative Five-Dose Testing Study

The five dose comparative CNS Cancer Cell Line cytotoxicity profiles of N9-[4'-Chloro-2'-butynyl-1'-yl]-2,6-dichloropurine 1, Bis-6,9-[4'-chloro-2'-butynyl-1'-yl]-thioguanine 2, Bis-6,9-[4'-chloro-2'-butynyl-1'-yl]-mercaptopurine 3, Bis-6,9-[[o-(chloromethyl) phenyl] methyl]-thioguanine 4, Bis-6,9-[[o-(chloromethyl) phenyl] methyl]-mercaptopurine 5, 6-[4'-chloro-2'-butynyl-1'-yl]-thioguanine 6, and N9-[4'-Chloro-2'-butynyl-1'-yl]-6-(4-methoxyphenyl) purine 7 are presented in this communication. These compounds were evaluated for cytotoxic activity against NCI-60 DTP human tumor cell line five dose screen. All the unsaturated highly lipophilic substituents as expected contributed for the excellent CNS cancer cell line cytotoxicity, GI(50) values 4-7 mu M. Further, the thioguanine, mercaptopurine, and 6-phenylpurine are identified as the potential candidates for the CNS active cancer drug development and to cross the blood brain barrier.