pubmed-article:11931625 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0226896 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0031327 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0205531 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0442027 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C1527415 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0441655 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0205177 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0038477 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0220825 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0056154 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
pubmed-article:11931625 | lifeskim:mentions | umls-concept:C1515655 | lld:lifeskim |
pubmed-article:11931625 | pubmed:issue | 8 | lld:pubmed |
pubmed-article:11931625 | pubmed:dateCreated | 2002-4-4 | lld:pubmed |
pubmed-article:11931625 | pubmed:abstractText | The synthesis and structure-activity relationship study of a series of compounds with heterocycles in place of the cis double bond in combretastatin A-4 (CA-4) are described. Substituted tosylmethyl isocyanides were found to be the key intermediates in construction of the heterocycles. Cytotoxicities of the heterocycle-based CA-4 analogues were evaluated against NCI-H460 and HCT-15 cancer cell lines. 3-Amino-4-methoxyphenyl and N-methyl-indol-5-yl were the best replacements for the 3-hydroxy-4-methoxyphenyl in CA-4. 4,5-Disubstituted imidazole was found to be the best for the replacement of the cis double bond in CA-4. Medicinal chemistry efforts led to the discovery of compounds 24h and 25f that were found to be 32 and 82% bioavailable, respectively, in rat. Evaluation of 24h and 25f against murine M5076 reticulum sarcoma in mice revealed that both compounds were orally efficacious with an increase in life span of 38.5 and 40.5%, respectively. | lld:pubmed |
pubmed-article:11931625 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11931625 | pubmed:language | eng | lld:pubmed |
pubmed-article:11931625 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11931625 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:11931625 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11931625 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11931625 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11931625 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11931625 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11931625 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11931625 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:11931625 | pubmed:month | Apr | lld:pubmed |
pubmed-article:11931625 | pubmed:issn | 0022-2623 | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:HuiYu-HuaYH | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:LiQunQ | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:WoodsKeith... | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:BarrKenneth... | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:CredoR... | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:MarshKennanK | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:FrostDavidD | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:ShamHing LHL | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:WangLeL | lld:pubmed |
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pubmed-article:11931625 | pubmed:author | pubmed-author:HannickSteven... | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:GherkeLauraL | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:WarnerRobertR | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:LeeJang YJY | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:Zielinski-Moz... | lld:pubmed |
pubmed-article:11931625 | pubmed:author | pubmed-author:RosenbergSaul... | lld:pubmed |
pubmed-article:11931625 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:11931625 | pubmed:day | 11 | lld:pubmed |
pubmed-article:11931625 | pubmed:volume | 45 | lld:pubmed |
pubmed-article:11931625 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:11931625 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:11931625 | pubmed:pagination | 1697-711 | lld:pubmed |
pubmed-article:11931625 | pubmed:dateRevised | 2007-11-15 | lld:pubmed |
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pubmed-article:11931625 | pubmed:year | 2002 | lld:pubmed |
pubmed-article:11931625 | pubmed:articleTitle | Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation. | lld:pubmed |
pubmed-article:11931625 | pubmed:affiliation | Global Pharmaceutical R & D, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064-6101, USA. le.wang@abbott.com | lld:pubmed |
pubmed-article:11931625 | pubmed:publicationType | Journal Article | lld:pubmed |
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