Aryl and Acyclic Unsaturated Derivatives of Thioguanine and 6-Mercaptopurine: Synthesis and Cytotoxic Activity

作者：Banh Tien N; Kode Nageswara R; Phadtare Shashikant^*

来源：Letters in Drug Design and Discovery, 2011, 8(8): 709-716.

• Substituted thioguanine
• Substituted 6-mercaptopurine
• Cytotoxic activity
• Thioguanine
• 6-mercaptopurine

A series of aryl and acyclic unsaturated chloromethyl derivatives of thioguanine and 6-mercaptopurine 1-20 were synthesized. These compounds were evaluated for cytotoxic activity against NCI-60 DTP human tumor cell line screen at 10 mu Molar concentration. Compound 1 exhibited potent cytotoxic activity with GI50 values 1 - 7 mu Molar range for most human tumor cell lines. Further, compounds 6, 9, 16 exhibited highly significant GI50 values 1 - 3 mu Molar range throghout the entire spectrum of the 60 cell line screen including the colon cancer and CNS cancer. Other compounds exhibited moderate activity.

• 出版日期2011-10