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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1988-11-17
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pubmed:abstractText |
A few 1-aryl 3-(2-chloroethyl)ureas (CEU) were synthesized and screened in vitro for their cytotoxicity. Some of these derivatives were assayed for their mutagenicity, their in vivo toxicity and their antineoplastic activity. Methyl 4-(p-(3-(2-chloroethyl) ureido) phenyl) butyrate, 4-methyl and 4-tertbutyl (3-(2-chloroethyl) ureido) phenyl) butyrate, 4-methyl and 4-tert-butyl (3-(2-chloroethyl) ureido) benzene had an ID50 of 28, 20 and 4 microM respectively when tested on LoVo cells, while chlorambucil (CBL) and CCNU had an ID50 of 21 and 45 microM. These 3 chloroethyl urea derivatives were not toxic when injected i.p. at doses up to 220 mg/kg, whereas chlorambucil was already toxic at 18.5 mg/kg. The survival time of BDF1 mice bearing L1210 leukemia tumors was significantly enhanced by intraperitoneal injections of CBL and CEU. The most cytotoxic derivative (tert-butyl derivative) gave the best antineoplastic activity with a median survival time 1.77 times that of the control at 10 mg/kg/day and was not toxic, whereas CBL at this concentration enhanced survival time by a factor of 1.6 and presented important side effects. The 4-tert-butyl (3-(2-chloroethyl) ureido) benzene and the methyl 4-(p-(3-(2-chloroethyl) ureido) phenyl) butyrate showed no mutagenicity when assayed on TA-97, TA-98, TA-100 and TA-102, four strains of S. thyphimurium, while CBL had a weak effect on TA-102 and CCNU was highly mutagenic on TA-100 and TA-102.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Chlorambucil,
http://linkedlifedata.com/resource/pubmed/chemical/Lomustine,
http://linkedlifedata.com/resource/pubmed/chemical/Nitrogen Mustard Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Phenylurea Compounds
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pubmed:status |
MEDLINE
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pubmed:issn |
0250-7005
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
595-8
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:3052247-Adenocarcinoma,
pubmed-meshheading:3052247-Animals,
pubmed-meshheading:3052247-Antineoplastic Agents,
pubmed-meshheading:3052247-Cell Line,
pubmed-meshheading:3052247-Cell Survival,
pubmed-meshheading:3052247-Chlorambucil,
pubmed-meshheading:3052247-Drug Screening Assays, Antitumor,
pubmed-meshheading:3052247-Humans,
pubmed-meshheading:3052247-Leukemia L1210,
pubmed-meshheading:3052247-Lomustine,
pubmed-meshheading:3052247-Mice,
pubmed-meshheading:3052247-Mutagenicity Tests,
pubmed-meshheading:3052247-Nitrogen Mustard Compounds,
pubmed-meshheading:3052247-Phenylurea Compounds,
pubmed-meshheading:3052247-Salmonella typhimurium,
pubmed-meshheading:3052247-Structure-Activity Relationship
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pubmed:articleTitle |
In vitro and in vivo activity of 1-aryl-3-(2-chloroethyl) urea derivatives as new antineoplastic agents.
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pubmed:affiliation |
Department of Biochemistry, Faculty of Medicine, Université Laval, Ste-Foy, Canada.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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