To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.

Abstract

Four ester prodrugs derived from the bifunctional alkylating agent chlorambucil, and one of its nitro-derivatives, 3-nitrochlorambucil conjugated to prasterone and pregnenolone, were synthesized and tested for their cytotoxic activity against eight human cell lines, using the standard MTT assay. A comparison between the esters and the controls, namely chlorambucil and 3-nitrochlorambucil would suggest that all four esters possess to varying degrees, specificity towards the breast adenocarcinoma cell line (MDA-mb468) than the other seven cells' lines tested. The overall findings are encouraging since it infers that these lipophilic esters not only have the ability to traverse specific cell membranes but also exhibit cytotoxicity towards most of the cell lines tested.

• Authors: Leroy A Shervington, Nigel Smith, Emma Norman, Timothy Ward, Roger Phillips, Amal Shervington
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 44 Issue 7 Pg. 2944-51 (Jul 2009) ISSN: 1768-3254 [Electronic] France
• PMID: 19121874 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Esters
• Nitro Compounds
• Chlorambucil
• Dehydroepiandrosterone
• Pregnenolone

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Chlorambucil (analogs & derivatives, chemical synthesis, pharmacology)
• Chromatography, High Pressure Liquid
• Dehydroepiandrosterone (chemistry)
• Esters (chemical synthesis, chemistry, pharmacology)
• Humans
• Inhibitory Concentration 50
• Neoplasms (pathology)
• Nitro Compounds (chemistry)
• Pregnenolone (chemistry)