Halogenated diarylacetylenes repress c-myc expression in cancer cells

  • Bioorg Med Chem Lett. 2014 Aug 1;24(15):3638-40. doi: 10.1016/j.bmcl.2014.04.113.
Vitaliy M Sviripa  1 ,  Wen Zhang  2 ,  Liliia M Kril  1 ,  Alice X Liu  1 ,  Yaxia Yuan  3 ,  Chang-Guo Zhan  4 ,  Chunming Liu  5 ,  David S Watt  6
Affiliations
  • 1. Department of Molecular and Cellular Biochemistry, College of Medicine, University of Kentucky, Lexington, KY 40536-0509, United States; Center for Pharmaceutical Research and Innovation, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, United States.
  • 2. Department of Molecular and Cellular Biochemistry, College of Medicine, University of Kentucky, Lexington, KY 40536-0509, United States; Lucille Parker Markey Cancer Center, University of Kentucky, Lexington, KY 40536-0093, United States.
  • 3. Center for Computational Drug Design, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, United States; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, United States.
  • 4. Center for Pharmaceutical Research and Innovation, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, United States; Center for Computational Drug Design, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, United States; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, United States.
  • 5. Department of Molecular and Cellular Biochemistry, College of Medicine, University of Kentucky, Lexington, KY 40536-0509, United States; Lucille Parker Markey Cancer Center, University of Kentucky, Lexington, KY 40536-0093, United States. Electronic address: [email protected].
  • 6. Department of Molecular and Cellular Biochemistry, College of Medicine, University of Kentucky, Lexington, KY 40536-0509, United States; Center for Pharmaceutical Research and Innovation, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, United States; Lucille Parker Markey Cancer Center, University of Kentucky, Lexington, KY 40536-0093, United States; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, United States. Electronic address: [email protected].
PMID: 24930834 DOI: 10.1016/j.bmcl.2014.04.113
Abstract

Halogenated diarylacetylenes that possess fluorine or chlorine substituents in one aryl ring and N-methylamino or N,N-dimethylamino in the Other aryl ring inhibit the proliferation of LS174T colon Cancer cells through the repression of c-Myc expression and induction of the cyclin-dependent kinase inhibitor-1 (i.e., p21(Wif1/Cip1)) and represent potentially useful antineoplastic agents.

Keywords
Antineoplastic agents; Colon cancer; Diarylacetylenes; c-myc.