2. Academic Validation
  3. Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma

Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma

  • J Med Chem. 2002 May 9;45(10):2116-9. doi: 10.1021/jm010926x.
Isabelle Giraud 1,  Maryse Rapp,  Jean-Claude Maurizis,  Jean-Claude Madelmont
Affiliations

Affiliation

  • 1 INSERM Unité 484, Rue Montalembert, BP 184, 63005 Clermont-Ferrand Cedex, France.
PMID: 11985479 DOI: 10.1021/jm010926x
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.

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