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

Leroy A. Shervington, Nigel Smith, Emma Norman, Timothy Ward, Roger Phillips, Amal Shervington

Research output: Contribution to journalArticle

24 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)2944-2951
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume44
Issue number7
Early online date9 Dec 2008
DOIs
Publication statusPublished - Jul 2009
Externally publishedYes

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Chlorambucil
Pregnenolone
Dehydroepiandrosterone
Cytotoxicity
Esters
Cells
Derivatives
Cell Line
Neoplasms
Alkylating Agents
Prodrugs
Cell membranes
Assays
Adenocarcinoma
Breast
Cell Membrane

Cite this

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title = "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.",
keywords = "Bifunctional alkylating agents, Cytotoxicity, Ester prodrugs, MTT assay, Prasterone, Pregnenolone",
author = "Shervington, {Leroy A.} and Nigel Smith and Emma Norman and Timothy Ward and Roger Phillips and Amal Shervington",
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To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines. / Shervington, Leroy A.; Smith, Nigel; Norman, Emma; Ward, Timothy; Phillips, Roger; Shervington, Amal.

In: European Journal of Medicinal Chemistry, Vol. 44, No. 7, 07.2009, p. 2944-2951.

Research output: Contribution to journalArticle

TY - JOUR

T1 - To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines

AU - Shervington, Leroy A.

AU - Smith, Nigel

AU - Norman, Emma

AU - Ward, Timothy

AU - Phillips, Roger

AU - Shervington, Amal

PY - 2009/7

Y1 - 2009/7

N2 - 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.

AB - 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.

KW - Bifunctional alkylating agents

KW - Cytotoxicity

KW - Ester prodrugs

KW - MTT assay

KW - Prasterone

KW - Pregnenolone

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