Synthesis and evaluation of substituted 4-(N-benzylamino)cinnamate esters as potential anti-cancer agents and HIV-1 integrase inhibitors

  • Bioorg Med Chem Lett. 2016 Aug 1;26(15):3810-2. doi: 10.1016/j.bmcl.2016.05.023.
Faridoon  1 ,  Adrienne L Edkins  2 ,  Michelle Isaacs  3 ,  Dumisani Mnkandhla  3 ,  Heinrich C Hoppe  4 ,  Perry T Kaye  5
Affiliations
  • 1. Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa.
  • 2. Department of Biochemistry and Microbiology, Rhodes University, Grahamstown 6140, South Africa; Biomedical Biotechnology Research Unit (BioBRU), Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
  • 3. Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
  • 4. Department of Biochemistry and Microbiology, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
  • 5. Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa. Electronic address: [email protected].
PMID: 27317645 DOI: 10.1016/j.bmcl.2016.05.023
Abstract

Encouraging selectivity and low micromolar activity against HeLa cervical carcinoma (IC50⩾3.0μM) and the aggressive MDA-MB-231 triple negative breast carcinoma (IC50⩾9.6μM) cell lines has been exhibited by a number of readily accessible 4-(N-benzylamino)cinnamate esters. The potential of the ligands as HIV-1 integrase inhibitors has also been examined.

Keywords
4-(N-Benzylamino)cinnamate esters; Anti-cancer agents; HIV-1 integrase inhibitors.