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

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

Volume: 8 Issue: 8

Author(s): Tien N. Banh, Nageswara R. Kode and Shashikant Phadtare

Affiliation:

Keywords: Substituted thioguanine, Substituted 6-mercaptopurine, Cytotoxic activity, Thioguanine, 6-mercaptopurine, HGPRT, MP, mercaptopurine, Selective substitution, DMF medium, leukemia, Non-Small Cell Lung Cancer, RPMI1640, Electrothermal MEL-TEMP appara-tus, Elemental analysis

Abstract: 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 10µ Molar concentration. Compound 1 exhibited potent cytotoxic activity with GI50 values 1 - 7 µ Molar range for most human tumor cell lines. Further, compounds 6, 9, 16 exhibited highly significant GI50 values 1 - 3 µ Molar range throghout the entire spectrum of the 60 cell line screen including the colon cancer and CNS cancer. Other compounds exhibited moderate activity.

Cite this article as:

N. Banh Tien, R. Kode Nageswara and Phadtare Shashikant, Aryl and Acyclic Unsaturated Derivatives of Thioguanine and 6- Mercaptopurine: Synthesis and Cytotoxic Activity, Letters in Drug Design & Discovery 2011; 8(8) . https://dx.doi.org/10.2174/157018011796576088