2. Academic Validation
  3. Searching for new derivatives of neocryptolepine: synthesis, antiproliferative, antimicrobial and antifungal activities

Searching for new derivatives of neocryptolepine: synthesis, antiproliferative, antimicrobial and antifungal activities

  • Eur J Med Chem. 2014 May 6:78:304-13. doi: 10.1016/j.ejmech.2014.03.060.
Katarzyna Sidoryk 1,  Anna Jaromin 2,  Jessica A Edward 3,  Marta Świtalska 4,  Joanna Stefańska 5,  Piotr Cmoch 6,  Joanna Zagrodzka 7,  Wojciech Szczepek 7,  Wanda Peczyńska-Czoch 8,  Joanna Wietrzyk 4,  Arkadiusz Kozubek 2,  Robert Zarnowski 3,  David R Andes 3,  Łukasz Kaczmarek 7
Affiliations

Affiliations

  • 1 Pharmaceutical Research Institute, Rydygiera 8, 01-793 Warsaw, Poland. Electronic address: k.sidoryk@ifarm.eu.
  • 2 Department of Lipids and Liposomes, Faculty of Biotechnology, University of Wroclaw, Przybyszewskiego 63/77, 51-148 Wroclaw, Poland.
  • 3 Department of Medicine, Section of Infectious Diseases, 4125 Microbial Sciences Building, 1550 Linden Dr., University of Wisconsin-Madison, Madison, WI 53706, USA.
  • 4 Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, 12 Weigla St., 53-114 Wroclaw, Poland.
  • 5 Medical University of Warsaw, Department of Pharmaceutical Microbiology, 3 Oczki St., 02-007 Warsaw, Poland.
  • 6 Pharmaceutical Research Institute, Rydygiera 8, 01-793 Warsaw, Poland; Institute of Organic Chemistry, Polish Academy of Sciences, Kasprzaka 44/52, 01-224 Warsaw, Poland.
  • 7 Pharmaceutical Research Institute, Rydygiera 8, 01-793 Warsaw, Poland.
  • 8 Division of Organic Technology, Faculty of Chemistry, Wroclaw University of Technology, Wybrzeze Wyspianskiego 27, 50-370 Wroclaw, Poland.
PMID: 24686017 DOI: 10.1016/j.ejmech.2014.03.060
Abstract

A series of novel amino acid and dipeptide derivatives of neocryptolepine were synthesized and tested for their antimicrobial, Antifungal and antiproliferative activity in vitro against Cancer cell lines (KB, A549, MCF-7, LoVo) and normal mice fibroblast cells (BALB/3T3). Biological evaluation revealed that almost all of the new compounds displayed high antiproliferative activity against the tested cells and moderate to potent Antibacterial activities. Interestingly, these compounds were active against Candida albicans biofilms at doses significantly lower than those required against free-floating planktonic Fungal cells. The most promising compounds are derivatives with glycine and L-proline as a substituent both at 2 and at 9 position of 5H-indolo[2,3-b]quinoline. In general, these new compounds (2a, 3a, 6a and 7a) showed the highest dual action against Cancer lines and infectious pathogenic microbes in vitro.

Keywords

Amino acid; Antimicrobial activity; Antiproliferative activity; Biofilm; NMR; Neocryptolepine; Peptide.

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