Abstract
The synthesis of a novel E-ring modified keto ether analogue of camptothecin and homocamptothecin by the cascade radical annulation route is reported. The analogue, Du1441, is an isomer of homocamptothecin, but includes the alpha-hydroxy carbonyl functionality that camptothecin possesses and homocamptothecin lacks. Despite these similarities, the new keto ether analogue is inactive in cell assays, and implications for the structure/activity relationship are discussed.
Publication types
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Research Support, Non-U.S. Gov't
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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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Camptothecin / analogs & derivatives*
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Camptothecin / chemical synthesis
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Camptothecin / pharmacology
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Chromatography, High Pressure Liquid
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Ethers / chemistry
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Humans
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Molecular Structure
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Spectrum Analysis
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents, Phytogenic
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Ethers
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Camptothecin