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1	Synthesis and Evaluation of Anibamine and Its Analogs as Novel Anti-Prostate Cancer Agents Haney, Kendra 24 November 2009 (has links) The chemokine receptor CCR5 has been implicated in the pathogenesis of prostate cancer. A novel natural product, anibamine, was isolated and found to be a micromolar inhibitor of the receptor. Anibamine was used as a new anti-prostate cancer lead compound. To discover the pharmacophore, analogs of anibamine were designed using the “deconstruction-reconstruction-elaboration” approach and synthesized. The establishment of a stereoselective route to only one isomer was explored, to increase yield and eliminate elaborate purification procedures. Analogs were found to have anti-prostate cancer activity at levels higher than the parent compound. The molecular modeling studies of the deconstructed analogs indicate that due to the psuedo-symmetry of the parent compound, the binding conformation of the deconstructed analogs may not be very different from each other. All this information together may help identify a next generation lead compound for anti-prostate cancer treatment. CCR5 Prostate Cancer Anibamine Synthesis Chemicals and Drugs Medicine and Health Sciences
2	SYNTHESIS AND BIOLOGICAL EVALUATION OF CCR5 ANTAGONISTS AS NOVEL ANTI-PROSTATE CANCER AGENTS Adams, Joanna Lee 01 January 2007 (has links) 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. PC-3 P69 M12 Anibamine CCL5 RANTES Prostate Cancer CCR5 DU-145 RT-PCR chemokine GOLD Chemicals and Drugs Medicine and Health Sciences

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Synthesis and Evaluation of Anibamine and Its Analogs as Novel Anti-Prostate Cancer Agents

SYNTHESIS AND BIOLOGICAL EVALUATION OF CCR5 ANTAGONISTS AS NOVEL ANTI-PROSTATE CANCER AGENTS