Abstract
Tetrahydroneotanshinlactone (TNT) and tetrahydronaphthalene-1-ol (TNO) derivatives were designed, synthesized, and evaluated for cytotoxic activity. The TNO derivatives were found to be a promising novel class of in vitro antitumor agents. The cyclohexene ring-A could dramatically affect the antitumor activity and selectivity. Compound 20 showed the highest potency with ED(50) values of 0.7 and 1.7 microM against SK-BR-3 and ZR-75-1 breast cancer cell lines, respectively.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Antineoplastic Agents, Phytogenic / pharmacology*
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Breast Neoplasms / drug therapy
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Cell Line, Tumor
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Cell Proliferation*
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Drug Design*
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Drug Resistance, Neoplasm
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Drug Screening Assays, Antitumor / methods
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Furans / pharmacology*
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Humans
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Lung Neoplasms / drug therapy
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Lung Neoplasms / pathology
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Mice
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Mice, Nude
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Molecular Structure
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Pyridazines*
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Pyrones / pharmacology*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Antineoplastic Agents, Phytogenic
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Furans
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Pyridazines
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Pyrones
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neotanshinlactone