Abstract
A diversity-oriented synthesis has been developed for facile construction of a library of carbohydrate-cyclopamine conjugates. The synthetic protocol is suitable for generating cyclopamine derivatives with various structural motifs for exploring the desired activity. From this initial library, we have observed one derivative that exhibits improved activity against lung cancer cell as compared to cyclopamine.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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Carbohydrates / chemical synthesis*
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Carbohydrates / pharmacology*
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Cell Line, Tumor
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Hedgehog Proteins / metabolism
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Humans
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Lung Neoplasms / drug therapy
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Lung Neoplasms / metabolism
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Structure-Activity Relationship
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Veratrum Alkaloids / chemical synthesis*
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Veratrum Alkaloids / pharmacology*
Substances
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Antineoplastic Agents
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Carbohydrates
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Hedgehog Proteins
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Veratrum Alkaloids
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cyclopamine