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Letters in Drug Design & Discovery


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

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

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

Volume 9 , Issue 5 , 2012

Page: [500 - 504] Pages: 5

DOI: 10.2174/157018012800389241

Price: $65


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, GI50 values 4-7 μM. 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.

Keywords: CNS, prostates, Cancer, leukemia, 60-cell lines, chemotherapeutic agents, breast cancer, metabolic pathways, proliferation, taxanes

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