Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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3-(Adamantan-1-yl)-4-hydroxybenzyl Substituted Purines and Pyrimidines: Synthesis and Cytotoxic Activity

Author(s): Nageswara Rao Kode, Dakshinamurthy Devangachinta, Shashikant Phadtare.

Abstract:

Selected adamantanyl purines and pyrimidines 1-10 were synthesized. These compounds were evaluated for cytotoxic activity against NCI-60 DTP human tumor cell line screen. N9-(3'-Adamantan-1-yl)-4'-hydroxy(benzyl)-2- amino-6-chloropurine, 3 and N9-[(3'-(Adamantan-1-yl)-4'-(2'',3'',4''-trifluorobenzyloxy)]benzyl-2-amino-6-chloropurine, 6 elicited significant cytotoxic activity with GI50 values in the 1–10 μM range for selected human tumor cell lines. While other compounds elicited moderate activity with GI50 values in the 10–20 μM range for most human tumor cell lines.

Keywords: Adamantan-1-yl-methylphenol, Cytotoxic activity, 2, 6, 9-substituted purines, 1, 4, 5-substituted pyrimidines, acid-catalyzed Friedel–Crafts alkylation, MEL-TEMP, Clofarabine, 3-adamantan-1-yl-4-hydroxybenzyl, Clofarabine, divergent fluorinated

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Article Details

VOLUME: 9
ISSUE: 10
Year: 2012
Page: [926 - 933]
Pages: 8
DOI: 10.2174/1570180811209050926
Price: $58