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Cytotoxicity and DNA binding property of triphenylethylene-coumarin hybrids with two amino side chains.

Abstract
Novel triphenylethylene-coumarin hybrids containing two amino side chains were designed and synthesized. Some of these 3,4-diphenyl coumarins, 7b-c (the double chains at 4-position on 3-,4-phenyl, respectively), and 13b-f (the double chains at 4-position on 3-phenyl and 7-position, respectively), showed a broad-spectrum and good anti-proliferative activity against five tumor cells and low cytotoxicity in osteoblast. UV-vis, fluorescence, and circular dichroism (CD) spectroscopies and thermal denaturation exhibited that compounds 7b (R=piperidinyl), 7e (R=NEt2), and 7f (R=4-methylpiperazinyl) had significant interactions with Ct-DNA by the intercalative mode of binding. Structure activity relationships (SARs) analysis suggested that the location of the two amino alkyl chains would play an important role both in the compounds against tumor cells proliferation and their interactions with DNA.
AuthorsLian Zhao, Yuchao Yao, Shuai Li, Mengjiao Lv, Hua Chen, Xiaoliu Li
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 24 Issue 3 Pg. 900-4 (Feb 01 2014) ISSN: 1464-3405 [Electronic] England
PMID24405706 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2013 Elsevier Ltd. All rights reserved.
Chemical References
  • Amino Acids
  • Coumarins
  • Stilbenes
  • DNA
  • coumarin
  • triphenylethylene
Topics
  • Amino Acids
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Cell Survival (drug effects)
  • Circular Dichroism
  • Coumarins (chemical synthesis, chemistry, pharmacology)
  • DNA (chemistry)
  • Drug Design
  • Humans
  • Stilbenes (chemical synthesis, chemistry, pharmacology)
  • Structure-Activity Relationship

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