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Defense Date


Document Type


Degree Name

Master of Science


Medicinal Chemistry

First Advisor

Dr. Yan Zhang


The chemokine receptor CCR5 has been implicated in the pathogenesis of prostate cancer (PCa). A novel series of piperazine derivatives have been designed and synthesized as CCR5 antagonists and their activity as inhibitors of PCa cell lines proliferation was explored. A lead compound has been identified which induced 100% inhibition of PCa cell proliferation at micromolar concentrations. Anibamine, the only natural product CCR5 antagonist, was also examined for its anti-proliferative activity and was found to inhibit proliferation of PCa cells at micromolar concentrations as well. The expression of RANTES mRNA was observed in DU-145, M12 and P69 cells via RT-PCR, while the expression of CCR5 mRNA was observed only in M12 cells. A CHO-CCR5 stable cell line was prepared for the CCR5 ligand competition binding assays. Both anibamine and the newly identified lead compound will serve as leads in the development of novel CCR5 antagonists as anti-prostate cancer agents.


Part of Retrospective ETD Collection, restricted to VCU only.


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Is Part Of

VCU University Archives

Is Part Of

VCU Theses and Dissertations

Date of Submission

June 2008