Source:http://linkedlifedata.com/resource/pubmed/id/12822184
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
2003-6-24
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pubmed:abstractText |
The substituted ethyl-2-phenacyl-3-phenylpyrrole-4-carboxylates were synthesized by a condensation of a beta-chloroenal and an alpha-aminoketone under neutral conditions. They proved to be potent cytotoxic agents against the growth of murine L1210 and P388 leukemias and human HL-60 promyelocytic leukemia, HuT-78 lymphoma, and HeLa-S(3) uterine carcinoma. Selective compounds were active against the growth of Tmolt(3) and Tmolt(4) leukemias and THP-1 acute monocytic leukemia, liver Hepe-2, ovary 1-A9, ileum HCT-8 adenocarcinoma, and osteosarcoma HSO. A mode of action study in HL-60 cells demonstrated that DNA and protein syntheses were inhibited after 60 min at 100 microM. DNA and RNA polymerases, PRPP-amido transferase, dihydrofolate reductase, thymidylate synthase, and TMP kinase activities were interfered with by the agent with reduction of d[NTP] pools. Nonspecific interaction with the bases of DNA and cross-linking of the DNA may play a role in the mode of action of these carboxylates.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0365-6233
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pubmed:author |
pubmed-author:ArgentiAnthonyA,
pubmed-author:BerkowitzJoshua DJD,
pubmed-author:BurnhamBruce SBS,
pubmed-author:DalglishGerard AGA,
pubmed-author:Durham JrRichard WRW,
pubmed-author:EvansMichael AMA,
pubmed-author:GuptonJohn TJT,
pubmed-author:HallIris HIH,
pubmed-author:HoffMafoloeM,
pubmed-author:HolubJustin MJM,
pubmed-author:KrumpeKeithK,
pubmed-author:ScarlettTanya CTC,
pubmed-author:SmithDaniel CDC,
pubmed-author:TaylorBrett MBM,
pubmed-author:WilsonDonna LDL
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pubmed:issnType |
Print
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pubmed:volume |
336
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
181-90
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12822184-Animals,
pubmed-meshheading:12822184-Antineoplastic Agents,
pubmed-meshheading:12822184-DNA Fragmentation,
pubmed-meshheading:12822184-Drug Screening Assays, Antitumor,
pubmed-meshheading:12822184-Enzyme Inhibitors,
pubmed-meshheading:12822184-Humans,
pubmed-meshheading:12822184-Mice,
pubmed-meshheading:12822184-Pyrroles,
pubmed-meshheading:12822184-Structure-Activity Relationship,
pubmed-meshheading:12822184-Tumor Cells, Cultured
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pubmed:year |
2003
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pubmed:articleTitle |
Synthesis and cytotoxicity of substituted ethyl 2-phenacyl-3-phenylpyrrole-4-carboxylates.
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pubmed:affiliation |
Department of Chemistry and Biochemistry, Rider University, Lawrenceville, NJ 08648, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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