Abstract
To enhance affinity for malignant cartilaginous tumors (chondrosarcomas), quaternary ammonium (QA) conjugates of chlorambucil and melphalan were prepared by linking the QA moiety to nitrogen mustards via an amide bond. They exhibited closely similar and sometimes more favorable values than their parent compounds. In the cell lines tested, the two QA conjugates displayed appreciable cytotoxicity, the QA conjugate of chlorambucil even showing an enhanced efficiency against chondrosarcoma compared with chlorambucil.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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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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Chlorambucil / chemistry*
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Chlorambucil / pharmacology
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Chondrosarcoma
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Drug Screening Assays, Antitumor
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Humans
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Melanoma
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Melphalan / chemistry*
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Mice
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Quaternary Ammonium Compounds / chemical synthesis*
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Quaternary Ammonium Compounds / chemistry
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Quaternary Ammonium Compounds / pharmacology
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Structure-Activity Relationship
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Tumor Cells, Cultured
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Tumor Stem Cell Assay
Substances
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Antineoplastic Agents
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Quaternary Ammonium Compounds
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Chlorambucil
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Melphalan