Abstract
The selective apoptosis-inducing activity of Amaryllidaceae alkaloids belonging to the crinane-type is reported. A mini-library of natural and synthetic crinane alkaloids was assembled. Biological screening indicated crinamine 4 and haemanthamine 9 to be potent inducers of apoptosis in tumour cells at micromolar concentrations. Structure-activity relationships demonstrated the requirement for both an alpha-C2 bridge and a free hydroxyl at the C-11 position as pharmacophoric requirements for this activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amaryllidaceae Alkaloids / chemistry
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Amaryllidaceae Alkaloids / isolation & purification
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Amaryllidaceae Alkaloids / pharmacology*
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Animals
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Antineoplastic Agents, Phytogenic / chemical synthesis
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Antineoplastic Agents, Phytogenic / chemistry
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Antineoplastic Agents, Phytogenic / isolation & purification
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Antineoplastic Agents, Phytogenic / pharmacology
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Apoptosis / drug effects*
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Cell Line
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Cell Line, Tumor
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Crinum*
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Dose-Response Relationship, Drug
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Humans
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Liliaceae / chemistry*
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Molecular Structure
Substances
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Amaryllidaceae Alkaloids
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Antineoplastic Agents, Phytogenic
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crinamine