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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Antitumor agents. 250. Design and synthesis of new curcumin analogues as potential anti-prostate cancer agents
Journal of Medicinal Chemistry, Volume 49, No. 13, Year 2006
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Description
In a continuing study of curcumin analogues as potential drug candidates to treat prostate cancer at both androgen-dependent and androgen-refractory stages, we designed and synthesized over 40 new analogues classified into four series: monophenyl analogues (series A), heterocycle-containing analogues (series B), analogues bearing various substituents on the phenyl rings (series C), and analogues with various linkers (series D). These new compounds were tested for cytotoxicity against two human prostate cancer cell lines, androgen-dependent LNCaP and androgen-independent PC-3. Antiandrogenic activity was also evaluated in LNCaP cells and PC-3 cells transfected with wild-type androgen receptor. Ten compounds possessed potent cytotoxicity against both LNCaP and PC-3 cells, seven only against LNCaP, and one solely against PC-3. This study established an advanced structure-activity relationship (SAR), and these correlations will guide the further design of new curcumin analogues with better anti-prostate cancer activity. © 2006 American Chemical Society.
Authors & Co-Authors
Nyarko, Alexander Kwadwo
United States, Chapel Hill
The University of North Carolina at Chapel Hill
Wu, Chinchung
United States, Chapel Hill
The University of North Carolina at Chapel Hill
Lee, Kuohsiung
United States, Chapel Hill
The University of North Carolina at Chapel Hill
Statistics
Citations: 166
Authors: 3
Affiliations: 1
Identifiers
Doi:
10.1021/jm051043z
ISSN:
00222623
Research Areas
Cancer