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Open AccessArticle

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

1
Department of Chemistry, Faculty of Science, Rhodes University, Grahamstown 6140, South Africa
2
Centre for Chemico and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa
3
Department of Biochemistry and Microbiology, Faculty of Science, Rhodes University, Grahamstown 6140, South Africa
4
School of Chemistry and Physics, Pietermaritzburg Campus, University of KwaZulu-Natal, Private Bag X01, Scottsville 3209, South Africa
5
Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Rhodes University, Grahamstown 6140, South Africa
*
Author to whom correspondence should be addressed.
Academic Editor: Andrew Tsotinis
Molecules 2020, 25(7), 1668; https://doi.org/10.3390/molecules25071668
Received: 21 March 2020 / Revised: 1 April 2020 / Accepted: 2 April 2020 / Published: 4 April 2020
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. View Full-Text
Keywords: arylpyrrole; chalcones; trypanosomiasis; Trypanosoma brucei; molecular hybridization arylpyrrole; chalcones; trypanosomiasis; Trypanosoma brucei; molecular hybridization
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MDPI and ACS Style

Zulu, A.I.; Oderinlo, O.O.; Kruger, C.; Isaacs, M.; Hoppe, H.C.; Smith, V.J.; Veale, C.G.L.; Khanye, S.D. Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives. Molecules 2020, 25, 1668.

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