Design, Synthesis and Biological Evaluation of Novel Acridine-Polyamine Conjugates Against Prostate Cancer

Hildebert B. Maurice, Rodger Phillips, Nazira Karodia

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

Prostate cancer is the most common cause of cancer death in men, aged 85 and over. Androgen receptor, a single polypeptide with three functional domains is very important during initiation and progression of the disease. In this study, a DNA intercalating agent, acridine is linked to the testosterone via a polyamine linker to obtain a compound with trifunctional characteristics, where the acridine intercalates the DNA, the polyamine linker binds the phosphoryl groups of the DNA backbone and the testosterone moiety binds into the AR ligand binding domain, with which its DNA binding domain is bound already to the DNA. This trifunctional compound and related derivatives have been synthesized and tested against androgen dependent- and androgen independent- prostate cancer cell lines and they have demonstrated to be cytotoxic at the micromolar concentrations.

Original languageEnglish
Pages (from-to)602-610
Number of pages9
JournalAfrican Journal of Pharmacy and Pharmacology
Volume3
Issue number12
Publication statusPublished - Dec 2009
Externally publishedYes

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Acridines
Polyamines
Prostatic Neoplasms
DNA
Androgens
Testosterone
Intercalating Agents
Androgen Receptors
Disease Progression
Cause of Death
Ligands
Cell Line
Peptides
Neoplasms

Cite this

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Design, Synthesis and Biological Evaluation of Novel Acridine-Polyamine Conjugates Against Prostate Cancer. / Maurice, Hildebert B.; Phillips, Rodger; Karodia, Nazira.

In: African Journal of Pharmacy and Pharmacology, Vol. 3, No. 12, 12.2009, p. 602-610.

Research output: Contribution to journalArticle

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