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
Letters in Drug Design & Discovery
Title:3-(Adamantan-1-yl)-4-hydroxybenzyl Substituted Purines and Pyrimidines: Synthesis and Cytotoxic Activity
Volume: 9 Issue: 10
Author(s): Nageswara Rao Kode, Dakshinamurthy Devangachinta and Shashikant Phadtare
Affiliation:
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
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.
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Rao Kode Nageswara, Devangachinta Dakshinamurthy and Phadtare Shashikant, 3-(Adamantan-1-yl)-4-hydroxybenzyl Substituted Purines and Pyrimidines: Synthesis and Cytotoxic Activity, Letters in Drug Design & Discovery 2012; 9 (10) . https://dx.doi.org/10.2174/1570180811209050926
DOI https://dx.doi.org/10.2174/1570180811209050926 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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