Abstract
A series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chemistry approach. All compounds were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA-MB-361), and colon adenocarcinoma (HT-29). Hexyl triazolyl-substituted 3-phenylpyrazolopyrimidine exhibited inhibition of Src kinase with an IC(50) value of 5.6 μM. 4-Methoxyphenyl triazolyl-substituted 3-phenylpyrazolopyrimidine inhibited the cell proliferation of HT-29 and SK-Ov-3 by 73% and 58%, respectively, at a concentration of 50 μM.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Breast Neoplasms / drug therapy
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Colonic Neoplasms / drug therapy
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Female
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Humans
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Inhibitory Concentration 50
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Models, Molecular
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Molecular Structure
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Ovarian Neoplasms / drug therapy
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Pyrans / chemistry*
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Pyrimidines / chemistry*
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Triazoles / chemistry*
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src-Family Kinases / antagonists & inhibitors
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src-Family Kinases / chemistry*
Substances
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Antineoplastic Agents
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Pyrans
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Pyrimidines
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Triazoles
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src-Family Kinases