Abstract
Two new series of 3-demethoxycarbonyl-3-ester and 3-demethoxycarbonyl-3-ether methyl anhydrovinblastine derivatives were designed, synthesized, and evaluated for their inhibitory activities against human non-small-cell lung cancer (A549) and cervical epithelial adenocarcinoma (HeLa) cell lines. Ester anhydrovinblastine derivatives exhibited potent cytotoxicity, whereas the ether analogues were much less active. The size of the introduced substituents was the foremost factor in determining the resultant cytotoxic activity. Compound 12b showed a similar cytotoxic potency to the positive control, anhydrovinblastine (1a).
Publication types
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Research Support, Non-U.S. Gov't
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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Combinatorial Chemistry Techniques
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Drug Screening Assays, Antitumor
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Esters
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Ethers / chemical synthesis
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Ethers / chemistry
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Ethers / pharmacology
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Female
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HeLa Cells
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Structure-Activity Relationship
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Vinblastine / analogs & derivatives*
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Vinblastine / chemical synthesis
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Vinblastine / chemistry
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Vinblastine / pharmacology
Substances
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Antineoplastic Agents
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Esters
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Ethers
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3',4'-anhydrovinblastine
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Vinblastine