Abstract
In vitro evaluation of the novel cycloalkyl-N-(4-chlorophenyl)-hydroxamic acids (2a-g) demonstrated that 2b,d,e exhibited rather marked inhibitory activity (IC50 = 7-10 microM) against pancreatic carcinoma, 2b-d against colon carcinoma, 2d against laryngeal carcinoma, and 2b,d against breast carcinoma. 2e showed the most pronounced anti-cytomegalovirus activity (EC50 = 1.5 and 0.8 microg mL(-1)) only at > or = 5-fold lower than the cytotoxic concentration. 2d and 2f showed modest, albeit selective, activity against cytomegalovirus (2d, EC50 = 7.3-8.9 microg mL(-1), selectivity index 7-10; 2f, EC50 = 7-13 microg mL(-1), selectivity index 10).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetamides / chemical synthesis*
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Acetamides / chemistry
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Acetamides / pharmacology
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Adamantane / analogs & derivatives*
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Adamantane / chemical synthesis*
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Adamantane / chemistry
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Adamantane / pharmacology
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Animals
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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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Antiviral Agents / chemical synthesis*
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology
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Cell Line
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Cell Line, Tumor
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Crystallography, X-Ray
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Cytomegalovirus / drug effects
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Drug Screening Assays, Antitumor
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Humans
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Hydroxamic Acids / chemical synthesis*
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Hydroxamic Acids / chemistry
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Hydroxamic Acids / pharmacology
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Mice
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Molecular Structure
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Structure-Activity Relationship
Substances
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Acetamides
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Antineoplastic Agents
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Antiviral Agents
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Hydroxamic Acids
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N-hydroxy-N-(4-chlorophenyl)adamantylformamide
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N-hydroxy-N-(4-chlorophenyl)cyclohexylacetamide
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Adamantane