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

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

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: P.Kaye@ru.ac.z.
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.

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