Molecules (Apr 2020)

Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives

  • Ayanda I. Zulu,
  • Ogunyemi O. Oderinlo,
  • Cuan Kruger,
  • Michelle Isaacs,
  • Heinrich C. Hoppe,
  • Vincent J. Smith,
  • Clinton G. L. Veale,
  • Setshaba D. Khanye

DOI
https://doi.org/10.3390/molecules25071668
Journal volume & issue
Vol. 25, no. 7
p. 1668

Abstract

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With an intention of identifying chalcone derivatives exhibiting anti-protozoal activity, a cohort of relatively unexplored arylpyrrole-based chalcone derivatives were synthesized in moderate to good yields. The resultant compounds were evaluated in vitro for their potential activity against a cultured Trypanosoma brucei brucei 427 strain. Several compounds displayed mostly modest in vitro anti-trypanosomal activity with compounds 10e and 10h emerging as active candidates with IC50 values of 4.09 and 5.11 µM, respectively. More importantly, a concomitant assessment of their activity against a human cervix adenocarcinoma (HeLa) cell line revealed that these compounds are non-toxic.

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