rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
2003-5-15
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pubmed:abstractText |
Novel substituted indolocarbazoles were synthesized, and their kinase inhibitory capability was evaluated in vitro. 6-Substituted indolocarbazoles 4 were found to be potent and selective D1/CDK4 inhibitors. 4d and 4h exhibited potent and ATP-competitive D1/CDK4 activities with IC50 values of 76 and 42 nM, respectively. Both compounds had high selectivity against the other kinases. These D1/CDK4 inhibitors inhibited tumor cell growth, arrested tumor cells at the G1 phase, and inhibited pRb phosphorylation.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/CDK4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Carbazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclin D1,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclin-Dependent Kinase 4,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclin-Dependent Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Proto-Oncogene Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Retinoblastoma Protein
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AndersonBryan DBD,
pubmed-author:BrooksHarold BHB,
pubmed-author:CampbellRobert MorrisRM,
pubmed-author:ConnerScott ESE,
pubmed-author:ConsidineEileenE,
pubmed-author:DempseyJack AJA,
pubmed-author:FaulMargaret MMM,
pubmed-author:LiTiechaoT,
pubmed-author:OggCathyC,
pubmed-author:PatelBharvinB,
pubmed-author:SchultzRichard MRM,
pubmed-author:ShihChuanC,
pubmed-author:SpencerCharles DCD,
pubmed-author:TeicherBeverlyB,
pubmed-author:WatkinsScott ASA,
pubmed-author:ZhouXunX,
pubmed-author:ZhuGuoxinG
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pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
46
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2027-30
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:12747775-Antineoplastic Agents,
pubmed-meshheading:12747775-Carbazoles,
pubmed-meshheading:12747775-Cell Division,
pubmed-meshheading:12747775-Cyclin D1,
pubmed-meshheading:12747775-Cyclin-Dependent Kinase 4,
pubmed-meshheading:12747775-Cyclin-Dependent Kinases,
pubmed-meshheading:12747775-Drug Screening Assays, Antitumor,
pubmed-meshheading:12747775-Enzyme Inhibitors,
pubmed-meshheading:12747775-G1 Phase,
pubmed-meshheading:12747775-Humans,
pubmed-meshheading:12747775-Indoles,
pubmed-meshheading:12747775-Phosphorylation,
pubmed-meshheading:12747775-Proto-Oncogene Proteins,
pubmed-meshheading:12747775-Retinoblastoma Protein,
pubmed-meshheading:12747775-Structure-Activity Relationship,
pubmed-meshheading:12747775-Tumor Cells, Cultured
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pubmed:year |
2003
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pubmed:articleTitle |
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.
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pubmed:affiliation |
Lilly Research Laboratories, A Division of Eli Lilly & Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA. Zhu_Guoxin@lilly.com
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pubmed:publicationType |
Journal Article
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