Abstract
Greater than the sum of its parts: Artemisinins are currently in phase I-II clinical trials against breast, colorectal and non-small-cell lung cancers. In an attempt to offer increased specificity, a series of hybrid artemisinin-polypyrrole minor groove binder conjugates are described. DNA binding/modelling studies and preliminary biological evaluation give insights into their mechanism of action and the potential of this strategy.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Combined Chemotherapy Protocols / chemical synthesis*
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Antineoplastic Combined Chemotherapy Protocols / chemistry
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Antineoplastic Combined Chemotherapy Protocols / pharmacology*
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Artemisinins / chemistry
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Artemisinins / pharmacology*
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Binding Sites / drug effects
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Cell Proliferation / drug effects
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DNA / chemistry
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DNA / drug effects*
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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HL-60 Cells
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HT29 Cells
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Humans
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Models, Molecular
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Molecular Conformation
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Molecular Dynamics Simulation
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Parasitic Sensitivity Tests
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Plasmodium falciparum / drug effects*
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Polymers / chemistry
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Polymers / pharmacology*
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Structure-Activity Relationship
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Thermodynamics
Substances
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Artemisinins
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Polymers
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Pyrroles
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polypyrrole
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DNA
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artemisinin