Abstract
Backbone degradable, linear, multiblock N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-doxorubicin (DOX) conjugates are synthesized by reversible addition-fragmentation chain transfer (RAFT) polymerization followed by chain extension via thiol-ene click reaction. The examination of molecular-weight-dependent antitumor activity toward human ovarian A2780/AD carcinoma in nude mice reveals enhanced activity of multiblock, second-generation, higher molecular weight conjugates when compared with traditional HPMA copolymer-DOX conjugates. The examination of body weight changes during treatment indicates the absence of non-specific adverse effects.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antibiotics, Antineoplastic / chemistry*
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Antibiotics, Antineoplastic / pharmacology*
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Body Weight / drug effects
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Doxorubicin / analogs & derivatives*
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Doxorubicin / chemical synthesis
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Doxorubicin / pharmacology
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Drug Carriers / chemistry*
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Drug Carriers / pharmacology
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Female
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Humans
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Mice
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Mice, Nude
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Molecular Weight
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Ovarian Neoplasms / drug therapy
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Polymethacrylic Acids / chemical synthesis*
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Polymethacrylic Acids / pharmacology*
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Structure-Activity Relationship
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Xenograft Model Antitumor Assays
Substances
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Antibiotics, Antineoplastic
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Drug Carriers
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Polymethacrylic Acids
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doxorubicin-N-(2-hydroxypropyl)methacrylamide copolymer conjugate
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Doxorubicin