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Synthesis and biological evaluation of dimeric furanoid macroheterocycles: discovery of new anticancer agents

Academic Article
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Overview

related to degree

  • Hale, Christopher (Kit) R H, Ph.D., Scripps Research 2009 - 2014

authors

  • Nicolaou, K.C.
  • Nilewski, C.
  • Hale, Christopher (Kit) R H
  • Ahles, C. F.
  • Chiu, C. A.
  • Ebner, C.
  • ElMarrouni, A.
  • Yang, L.
  • Stiles, K.
  • Nagrath, D.

publication date

  • 2015

journal

  • Journal of the American Chemical Society  Journal

abstract

  • A recently developed dimerization/macrocyclization was employed to synthesize a series of macroheterocycles which were biologically evaluated, leading to the discovery of a number of potent cytotoxic agents (e.g., 27: GI50 = 51 nM against leukemia CCRF-CEM cell line; 29: GI50 = 99 nM against melanoma MDA-MB-435 cell line). Further biological studies support an apoptosis mechanism of action for these compounds involving deregulation of the tricarboxylic acid cycle activity and suppression of mitochondrial function in cancer cells.

subject areas

  • Antineoplastic Agents
  • Apoptosis
  • Cell Line, Tumor
  • Chemistry Techniques, Synthetic
  • Dimerization
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Furans
  • Heterocyclic Compounds
  • Humans
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Identity

International Standard Serial Number (ISSN)

  • 0002-7863

Digital Object Identifier (DOI)

  • 10.1021/jacs.5b00141

PubMed ID

  • 25827338
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Additional Document Info

start page

  • 4766

end page

  • 4770

volume

  • 137

issue

  • 14

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