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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 8, Issue 8, 2011

Page: [709 - 716] Pages: 8

DOI: 10.2174/157018011796576088

Price: $65


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.

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

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