|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0003392,
umls-concept:C0205198,
umls-concept:C0205314,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0522529,
umls-concept:C0678594,
umls-concept:C0679622,
umls-concept:C1707689,
umls-concept:C1883254
|
|
pubmed:issue |
17
|
|
pubmed:dateCreated |
2008-9-4
|
|
pubmed:abstractText |
A series of hydroxamic acids with conjugated structure was designed and synthesized to explore the possible HDAC subtype selectivity by testing these compounds against recombinant human HDAC1 and HDAC4. The most selective compound resulted 5a, with a SI of 11.9. The enzymatic inhibitory activity of these conjugated compounds was relatively weak; however, some of these compounds showed significant effect in inducing apoptosis. Moreover, the anti-proliferative activity in cancer cells resulted quite promising, especially in the HCT119 cell line.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclin-Dependent Kinase Inhibitor...,
http://linkedlifedata.com/resource/pubmed/chemical/HDAC1 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/HDAC4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Histone Deacetylase 1,
http://linkedlifedata.com/resource/pubmed/chemical/Histone Deacetylases,
http://linkedlifedata.com/resource/pubmed/chemical/Hydroxamic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Repressor Proteins
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Sep
|
|
pubmed:issn |
1464-3391
|
|
pubmed:author |
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
1
|
|
pubmed:volume |
16
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
7992-8002
|
|
pubmed:dateRevised |
2009-11-19
|
|
pubmed:meshHeading |
pubmed-meshheading:18701301-Animals,
pubmed-meshheading:18701301-Antineoplastic Agents,
pubmed-meshheading:18701301-Apoptosis,
pubmed-meshheading:18701301-Binding Sites,
pubmed-meshheading:18701301-Blotting, Western,
pubmed-meshheading:18701301-Cell Cycle,
pubmed-meshheading:18701301-Cell Differentiation,
pubmed-meshheading:18701301-Cell Proliferation,
pubmed-meshheading:18701301-Cyclin-Dependent Kinase Inhibitor p21,
pubmed-meshheading:18701301-Drug Design,
pubmed-meshheading:18701301-Drug Screening Assays, Antitumor,
pubmed-meshheading:18701301-Enzyme Activation,
pubmed-meshheading:18701301-Histone Deacetylase 1,
pubmed-meshheading:18701301-Histone Deacetylases,
pubmed-meshheading:18701301-Humans,
pubmed-meshheading:18701301-Hydroxamic Acids,
pubmed-meshheading:18701301-Ligands,
pubmed-meshheading:18701301-Molecular Structure,
pubmed-meshheading:18701301-Recombinant Proteins,
pubmed-meshheading:18701301-Repressor Proteins,
pubmed-meshheading:18701301-Stereoisomerism,
pubmed-meshheading:18701301-Structure-Activity Relationship,
pubmed-meshheading:18701301-Time Factors,
pubmed-meshheading:18701301-Tumor Cells, Cultured
|
|
pubmed:year |
2008
|
|
pubmed:articleTitle |
Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents.
|
|
pubmed:affiliation |
Department of Medicinal Chemistry, China Pharmaceutical University, People's Republic of China.
|
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|
