Literature DB >> 19121874

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 Shervington1, Nigel Smith, Emma Norman, Timothy Ward, Roger Phillips, Amal Shervington.   

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.

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Year:  2008        PMID: 19121874     DOI: 10.1016/j.ejmech.2008.11.014

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Investigating the Stability of Six Phenolic TMZ Ester Analogues, Incubated in the Presence of Porcine Liver Esterase and Monitored by HPLC.

Authors:  Leroy A Shervington; Oliver Ingham
Journal:  Molecules       Date:  2022-05-05       Impact factor: 4.927

2.  A novel series of phenolic temozolomide (TMZ) esters with 4 to 5-fold increased potency, compared to TMZ, against glioma cells irrespective of MGMT expression.

Authors:  Leroy Shervington; Oliver Ingham; Amal Shervington
Journal:  RSC Adv       Date:  2020-05-06       Impact factor: 4.036

3.  Synthesis and Evaluation of New Potential Benzo[a]phenoxazinium Photosensitizers for Anticancer Photodynamic Therapy.

Authors:  Juan Zhang; Wellington Tavares de Sousa Júnior; Victor Carlos Mello da Silva; Mosar Correa Rodrigues; José Athayde Vasconcelos Morais; Jia-Li Song; Zhi-Qiang Cheng; João Paulo Figueiró Longo; Ricardo Bentes Azevedo; Cheng-Shi Jiang; Luís Alexandre Muehlmann; Hua Zhang
Journal:  Molecules       Date:  2018-06-13       Impact factor: 4.411

  3 in total

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