Linked Life Data

21345671

Source:http://linkedlifedata.com/resource/pubmed/id/21345671

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
2011-3-14
pubmed:abstractText
Thirteen hydroxyethyl- analogs of combretastatin A-4 (CA-4) that contain the 1-(1'-hydroxyethyl)-1-(3",4",5"-trimethoxyphenyl)-2-(substituted phenyl)ethene framework were synthesized. Molecular modeling studies at the DFT level showed that compound 3j adopts a 'twisted' conformation mimicking CA-4. The cytotoxicity of the novel compounds against the growth of murine B16 melanoma and L1210 lymphoma cells in culture was measured using an MTT assay. Three analogs 3f, 3h, and 3j were active. Of these, 3j, which has the same substituents as CA-4 and IC(50) values of 16.1 and 4.1 ?M against B16 and L1210 cells, respectively, was selected for further biological evaluation. The activity of 3j was verified by the NCI 60 cell line screen. Compound 3j causes microtubule depolymerization in A-10 cells with an EC(50) of 21.2 ?M. Analog 3j, which has excellent water solubility of 479 ?M, had antitumor activity in a syngeneic L1210 murine model.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
1464-3405
pubmed:author
pubmed:copyrightInfo
Copyright © 2011 Elsevier Ltd. All rights reserved.
pubmed:issnType
Electronic
pubmed:day
1
pubmed:volume
21
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2087-91
pubmed:meshHeading
pubmed:year
2011
pubmed:articleTitle
Design and synthesis of novel enhanced water soluble hydroxyethyl analogs of combretastatin A-4.
pubmed:affiliation
Department of Chemistry, Division of Natural and Applied Sciences, Hope College, Holland, MI 49422, USA.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't