2. Academic Validation
  3. Improved anticancer and antiparasitic activity of new lawsone Mannich bases

Improved anticancer and antiparasitic activity of new lawsone Mannich bases

  • Eur J Med Chem. 2017 Jan 27:126:421-431. doi: 10.1016/j.ejmech.2016.11.043.
Katharina Mahal 1,  Aamir Ahmad 2,  Florian Schmitt 1,  Julia Lockhauserbäumer 3,  Kathrin Starz 3,  Rohan Pradhan 4,  Subhash Padhye 4,  Fazlul H Sarkar 2,  Waleed S Koko 5,  Rainer Schobert 1,  Klaus Ersfeld 3,  Bernhard Biersack 6
Affiliations

Affiliations

  • 1 Organic Chemistry Laboratory, University of Bayreuth, Universitaetsstrasse 30, 95440 Bayreuth, Germany.
  • 2 Karmanos Cancer Institute, Dept. of Pathology, Wayne State University, Detroit 48201, USA.
  • 3 Laboratory of Molecular Parasitology, Department of Genetics, University of Bayreuth, 95440 Bayreuth, Germany.
  • 4 Department of Chemistry, Abeda Inamdar Senior College, Pune 411001, India.
  • 5 Department of Microbiology and Parasitology, Medicinal and Aromatic Plants Research Institute, National Centre for Research, Khartoum, Sudan; College of Science and Arts (Ar Rass), Qassim University, Buraidah, Saudi Arabia.
  • 6 Organic Chemistry Laboratory, University of Bayreuth, Universitaetsstrasse 30, 95440 Bayreuth, Germany. Electronic address: bernhard.biersack@yahoo.com.
PMID: 27912173 DOI: 10.1016/j.ejmech.2016.11.043
Abstract

Substituted lawsone Mannich Bases 2a-e, 3a-e and 4a-e were prepared and tested for their biological activities. The new fatty alkyl substituted compounds 2a-c exhibited strong and selective growth inhibitory activities in the low one-digit micromolar and sub-micromolar range against a panel of human Cancer cell lines associated with ROS formation. In addition, compounds 2a-c revealed sub-micromolar anti-trypanosomal activities against parasitic Trypanosoma brucei brucei cells via deformation of the microtubule Cytoskeleton. The N-hexadecyl compound 2c was also highly active against locally isolated Entamoeba histolytica Parasite samples exceeding the activity of metronidazole.

Keywords

Anticancer drugs; Antiparasitic drugs; Lawsone; Mannich base.

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