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Free radical scavenging and antiproliferative properties of Biginelli adducts.

Abstract
A series of Biginelli adducts bearing different substituents at C-4 position were synthesized by using p-sulfonic acid calix[4]arene as a catalyst. The in vitro potential to scavenge reactive nitrogen/oxygen species (RNS and ROS) and the ability to inhibit cancer cells growth were then investigated. Four adducts were found to be potent scavengers of 2,2-diphenyl-1-picrylhydrazyl (RNS) and/or superoxide anion (ROS) radicals. The antiproliferative activity against cancer cells was disclosed for the first time for 16 monastrol analogs. The capacity of all compounds to inhibit cancer cells growth was dependent on the histological origin of cells, except for BA24, which was highly active against all cell lines. BA20 and BA33 were as potent as the reference drug doxorubicin against adriamycin-resistant ovarian and prostate cancer cells, respectively. These results highlight some monastrol analogs as lead compounds for the design of new free radical scavengers and anticancer agents.
AuthorsDaniel L da Silva, Fabiano S Reis, Dandara R Muniz, Ana Lúcia T G Ruiz, João E de Carvalho, Adão A Sabino, Luzia V Modolo, Angelo de Fátima
JournalBioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 20 Issue 8 Pg. 2645-50 (Apr 15 2012) ISSN: 1464-3391 [Electronic] England
PMID22410248 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2012 Elsevier Ltd. All rights reserved.
Chemical References
  • Antineoplastic Agents
  • Biphenyl Compounds
  • Free Radical Scavengers
  • Picrates
  • 1,1-diphenyl-2-picrylhydrazyl
Topics
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Biphenyl Compounds (chemical synthesis, chemistry, pharmacology)
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Free Radical Scavengers (chemical synthesis, chemistry, pharmacology)
  • Humans
  • Molecular Structure
  • Picrates (chemical synthesis, chemistry, pharmacology)
  • Structure-Activity Relationship

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