1. Academic Validation
  2. Halogenated diarylacetylenes repress c-myc expression in cancer cells

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

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: chunming.liu@uky.edu.
  • 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: dwatt@uky.edu.
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.

Figures