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

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

Journal Name: Letters in Drug Design & Discovery

Volume 8 , Issue 8 , 2011

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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.

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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Article Details

VOLUME: 8
ISSUE: 8
Year: 2011
Page: [709 - 716]
Pages: 8
DOI: 10.2174/157018011796576088
Price: $65

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