A comparative assessment of a-lipoic acid N-phenylamides as non-steroidal androgen receptor antagonists both on and off gold nanoparticles
Data(s) |
01/01/2012
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Resumo |
A group of α-lipoic acid N-phenylamides were synthesized employing a variety of amide coupling protocols utilizing electron deficient anilines. These compounds were then assessed for their ability to block androgen-stimulated proliferation of a human prostate cancer cell line, LNCaP. These structurally simple compounds displayed anti-proliferative activities at, typically, 5–20 μM concentrations and were comparable to a commonly used anti-androgen Bicalutamide®. The inclusion of a disulfide (RS-SR) moiety, serving as an anchor to several metal nanoparticle systems (Au, Ag, Fe<sub>2</sub>O<sub>3</sub>, etc.), does not impede any biological activity. Conjugation of these compounds to a gold nanoparticle surface resulted in a high degree of cellular toxicity, attributed to the absence of a biocompatible group such as PEG within the organic scaffold. |
Identificador | |
Idioma(s) |
eng |
Publicador |
Academic Press |
Relação |
http://dro.deakin.edu.au/eserv/DU:30047076/henderson-comparativeassessment-2012.pdf http://dx.doi.org/10.1016/j.bioorg.2011.11.007 |
Direitos |
2011, Elsevier |
Palavras-Chave | #α-Lipoic acid #androgen receptor #bicalutamide #flutamide #prostate cancer |
Tipo |
Journal Article |