Abstract
A series of novel macrocyclic taxoids was designed and synthesized by connecting the C-2 and C-3' N positions of the taxoid framework with various tethers. Cytotoxicity of these macrocyclic taxoids was evaluated against a human breast cancer cell line LCC6-WT, and a couple of the taxoids exhibited 0.09-0.3 microM IC(50) values.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Antineoplastic Agents, Phytogenic / chemical synthesis*
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Antineoplastic Agents, Phytogenic / pharmacology*
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Breast Neoplasms / drug therapy
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Cell Survival / drug effects
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Crystallography, X-Ray
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Drug Design
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Drug Screening Assays, Antitumor
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Female
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Humans
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Indicators and Reagents
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Molecular Conformation
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Paclitaxel / analogs & derivatives*
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Paclitaxel / chemical synthesis
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Paclitaxel / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents, Phytogenic
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Indicators and Reagents
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Paclitaxel