Linked Life Data

19645447

Source:http://linkedlifedata.com/resource/pubmed/id/19645447

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
16
pubmed:dateCreated
2010-6-21
pubmed:abstractText
Nineteen new phenanthrene-based tylophorine analogues with various functional groups on the piperidine moiety were designed, synthesized, and evaluated for in vitro anticancer activity against four human tumor cell lines. Analogues 15 and 21 showed approximately 2-fold enhanced inhibitory activity as compared with our prior lead compound (PBT-1). Analogues 23 and 24 with S- and R-configured substituents, respectively, at the piperidine 3'-position exhibited comparable cytotoxicity to that of PBT-1. Furthermore, mechanistic studies to investigate the effects of the new compounds on Akt protein in lung cancer cells and the NF-kB signaling pathway suggested that the compounds may exert their inhibitory activity on tumor cells through inhibition of activation of both Akt and NF-kB signaling pathway.
pubmed:grant
pubmed:commentsCorrections
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
1520-4804
pubmed:author
pubmed:issnType
Electronic
pubmed:day
27
pubmed:volume
52
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
5262-8
pubmed:dateRevised
2011-4-22
pubmed:meshHeading
pubmed-meshheading:19645447-Alkaloids, pubmed-meshheading:19645447-Antineoplastic Agents, pubmed-meshheading:19645447-Cell Line, Tumor, pubmed-meshheading:19645447-Drug Design, pubmed-meshheading:19645447-Drug Screening Assays, Antitumor, pubmed-meshheading:19645447-Humans, pubmed-meshheading:19645447-Indoles, pubmed-meshheading:19645447-Indolizines, pubmed-meshheading:19645447-Models, Molecular, pubmed-meshheading:19645447-Molecular Conformation, pubmed-meshheading:19645447-NF-kappa B, pubmed-meshheading:19645447-Phenanthrenes, pubmed-meshheading:19645447-Phenanthrolines, pubmed-meshheading:19645447-Piperidines, pubmed-meshheading:19645447-Proto-Oncogene Proteins c-akt, pubmed-meshheading:19645447-Signal Transduction, pubmed-meshheading:19645447-Stereoisomerism, pubmed-meshheading:19645447-Structure-Activity Relationship
pubmed:year
2009
pubmed:articleTitle
Antitumor agents 268. Design, synthesis, and mechanistic studies of new 9-substituted phenanthrene-based tylophorine analogues as potent cytotoxic agents.
pubmed:affiliation
Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7568, USA. qshi1@email.unc.edu
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't, Research Support, N.I.H., Extramural