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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
22
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pubmed:dateCreated |
2004-10-14
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pubmed:abstractText |
Two closely related diaryl acylsulfonamides were recently reported as potent antitumor agents against a broad spectrum of human tumor xenografts (colon, lung, breast, ovary, and prostate) in nude mice. Especially intriguing was their activity against colorectal cancer xenografts. In this paper, rapid parallel synthesis along with traditional medicinal chemistry techniques were used to quickly delineate the structure-activity relationships of the substitution patterns in both phenyl rings of the acylsufonamide anti-proliferative scaffold. Although the molecular target of the compounds remains unclear, we determined that the vascular endothelial growth factor-dependent human umbilical vein endothelial cells assay in combination with a soft agar disk diffusion assay allowed for optimization of potency in the series. The pharmacokinetic properties and in vivo activity in an HCT116 xenograft model are reported for representative compounds.
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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 |
Oct
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AikinsJames AJA,
pubmed-author:AlvarezEnriqueE,
pubmed-author:CabrejasLuisa M MartinLM,
pubmed-author:CheungYiu-YinYY,
pubmed-author:ConsidineEileen LEL,
pubmed-author:De DiosAlfonsoA,
pubmed-author:DurstGregory LGL,
pubmed-author:FerrittoRafaelR,
pubmed-author:GieraDeborah DDD,
pubmed-author:GrossmanCora SueCS,
pubmed-author:HipskindPhilip APA,
pubmed-author:HollisterBeth ABA,
pubmed-author:HuangZhongpingZ,
pubmed-author:IversenPhilip WPW,
pubmed-author:LawKevin LKL,
pubmed-author:LiTiechaoT,
pubmed-author:LinHo-ShenHS,
pubmed-author:LobbKaren LKL,
pubmed-author:LopezBeatrizB,
pubmed-author:LopezJose EJE,
pubmed-author:MaderMary MMM,
pubmed-author:McCannDenis JDJ,
pubmed-author:MoleroVictorianoV,
pubmed-author:ReillyJohn EJE,
pubmed-author:RichettMichael EME,
pubmed-author:ShihChuanC,
pubmed-author:TeicherBeverlyB,
pubmed-author:WhiteWesley TWT,
pubmed-author:WikelJames HJH
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pubmed:issnType |
Print
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pubmed:day |
21
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pubmed:volume |
47
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5367-80
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15481975-Animals,
pubmed-meshheading:15481975-Antineoplastic Agents,
pubmed-meshheading:15481975-Cell Division,
pubmed-meshheading:15481975-Cell Line,
pubmed-meshheading:15481975-Drug Screening Assays, Antitumor,
pubmed-meshheading:15481975-Endothelium, Vascular,
pubmed-meshheading:15481975-Female,
pubmed-meshheading:15481975-Half-Life,
pubmed-meshheading:15481975-Humans,
pubmed-meshheading:15481975-Mice,
pubmed-meshheading:15481975-Mice, Nude,
pubmed-meshheading:15481975-Quantitative Structure-Activity Relationship,
pubmed-meshheading:15481975-Rats,
pubmed-meshheading:15481975-Rats, Inbred F344,
pubmed-meshheading:15481975-Sulfonamides,
pubmed-meshheading:15481975-Transplantation, Heterologous,
pubmed-meshheading:15481975-Umbilical Veins,
pubmed-meshheading:15481975-Vascular Endothelial Growth Factor A
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pubmed:year |
2004
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pubmed:articleTitle |
Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
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pubmed:affiliation |
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA. Lobb_Karen@Lilly.com
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pubmed:publicationType |
Journal Article,
In Vitro
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