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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
21
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pubmed:dateCreated |
2010-10-11
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pubmed:abstractText |
Prodrugs have proven to be very useful in enhancing aqueous solubility of sparingly water-soluble drugs, thereby increasing in vivo efficacy without a need of special excipients. In vitro and in vivo evaluations of a number of amino acid prodrugs of 1, a previously identified potent tubulin polymerization inhibitor and cytotoxic against various cancer cell lines led to the discovery of 3·HCl (l-valine attached) which is highly efficacious in mouse xenografts bearing human cancer. Pharmacokinetic analysis in rats revealed that compound 1 was released immediately upon administration of 3·HCl intravenously, with rapid clearance of 3·HCl indicating the effective cleavage of prodrug. Compound 3·HCl (CKD-516) has now been progressed to phase 1 clinical trial.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AhnSoon KilSK,
pubmed-author:BaeSuyealS,
pubmed-author:ChoiHojinH,
pubmed-author:ChoiNam SongNS,
pubmed-author:KimDal-HyunDH,
pubmed-author:KimSoo JinSJ,
pubmed-author:KimYoung HoonYH,
pubmed-author:LeeJaekwangJ,
pubmed-author:LeeKyung JooKJ,
pubmed-author:LeeSeo-HeeSH,
pubmed-author:LeeSungsookS,
pubmed-author:MoonSeung KeeSK,
pubmed-author:ParkGyu TaeGT
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pubmed:copyrightInfo |
Copyright © 2010. Published by Elsevier Ltd.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6327-30
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pubmed:meshHeading |
pubmed-meshheading:20850313-Animals,
pubmed-meshheading:20850313-Antineoplastic Agents,
pubmed-meshheading:20850313-Benzophenones,
pubmed-meshheading:20850313-Cell Proliferation,
pubmed-meshheading:20850313-HL-60 Cells,
pubmed-meshheading:20850313-Humans,
pubmed-meshheading:20850313-Injections, Intravenous,
pubmed-meshheading:20850313-Male,
pubmed-meshheading:20850313-Mice,
pubmed-meshheading:20850313-Mice, Inbred BALB C,
pubmed-meshheading:20850313-Prodrugs,
pubmed-meshheading:20850313-Rats,
pubmed-meshheading:20850313-Rats, Sprague-Dawley,
pubmed-meshheading:20850313-Solubility,
pubmed-meshheading:20850313-Tubulin,
pubmed-meshheading:20850313-Tubulin Modulators,
pubmed-meshheading:20850313-Water,
pubmed-meshheading:20850313-Xenograft Model Antitumor Assays
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pubmed:year |
2010
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pubmed:articleTitle |
Discovery of a potent tubulin polymerization inhibitor: synthesis and evaluation of water-soluble prodrugs of benzophenone analog.
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pubmed:affiliation |
Chong Kun Dang Research Institute, CKD Pharmaceuticals Inc., PO Box 74, Chonan, Republic of Korea.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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