Journal ArticleDOI
Novel Schiff base copper complexes of quinoline-2 carboxaldehyde as proteasome inhibitors in human prostate cancer cells.
Shreelekha Adsule,Vivek Barve,Di Chen,Fakhara Ahmed,Q. Ping Dou,Subhash Padhye,Fazlul H. Sarkar +6 more
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TLDR
It is found that quinoline thiosemicarbazone 2 was the most potent and inhibited proteosome activity in intact human prostate cancer PC-3 and LNCaP cells (IC50 of 4 and 3.2 microM, respectively) compared to clioquinol and pyrrolidine dithiocarbamate.Abstract:
We report the synthesis of novel 1:1 Schiff base copper complexes of quinoline-2-carboxaldehyde showing dose-dependent, antiproliferative, and proapoptotic activity in PC-3 and LNCaP prostate cancer cells. We found that quinoline thiosemicarbazone 2 (FPA-137) was the most potent and inhibited proteosome activity in intact human prostate cancer PC-3 and LNCaP cells (IC50 of 4 and 3.2 microM, respectively) compared to clioquinol and pyrrolidine dithiocarbamate (IC50 of 10 and 20 microM), supporting the novelty of 2.read more
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Advances in copper complexes as anticancer agents.
Carlo Santini,Maura Pellei,Valentina Gandin,Marina Porchia,Francesco Tisato,Cristina Marzano +5 more
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Copper complexes as anticancer agents
TL;DR: This overview, collecting the most significant strategies adopted in the last ten years to design promising anticancer copper(I,II) compounds, would be a help to the researchers working in this field.
Journal ArticleDOI
Copper in diseases and treatments, and copper-based anticancer strategies.
TL;DR: Investigations into the occurrence of mechanisms of action quite different from platinum drugs head toward the development of new anticancer metallodrugs with improved specificity and decreased toxic side effects.
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A review on anticancer potential of bioactive heterocycle quinoline.
TL;DR: This review has compiled and discussed specifically the anticancer potential of quinoline derivatives, which could provide a low-height flying bird's eye view of theQuinoline derived compounds to a medicinal chemist for a comprehensive and target oriented information for development of clinically viable anticancer drugs.
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Quinoline as a Privileged Scaffold in Cancer Drug Discovery
Solomon Vr,Hoyun Lee +1 more
TL;DR: In vitro and in vivo anticancer activities of quinoline and its analogs are focused on in the context of cancer drug development and refinement, and selective and specific activity against various cancer drug targets are reviewed.
References
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The use of conductivity measurements in organic solvents for the characterisation of coordination compounds
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Ubiquitin, proteasomes, and the regulation of intracellular protein degradation.
TL;DR: The complexity of the ubiquitin system is reflected in the broad range of processes it regulates; these include key steps in cell cycle progression, processing of foreign proteins for presentation by class I MHC molecules, and the control of cell proliferation.
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Copper(II) Complexes with Subnormal Magnetic Moments
TL;DR: In this paper, a review of subnormal magnetic moments of copper(II) compounds with subnormal magnet moments can be found, which can be roughly divided into two types: those with direct copper-to-copper interaction and those with super-exchange interaction.
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Proteasome Inhibition Measurements: Clinical Application
Eric S. Lightcap,Teresa A. McCormack,Christine S. Pien,Vincent Chau,Julian Adams,Peter J. Elliott +5 more
TL;DR: The described assay provides a reliable method for studying the pharmacodynamics of proteasome inhibitors and is now in use in concurrent phase I clinical trials with PS-341.
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Clioquinol and pyrrolidine dithiocarbamate complex with copper to form proteasome inhibitors and apoptosis inducers in human breast cancer cells
TL;DR: The feature of breast cancer cells and tissues to accumulate copper can be used as a targeting method for anticancer therapy through treatment with novel compounds such as CQ and PDTC that become active proteasome inhibitors and breast cancer cell killers in the presence of copper.