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

• Main Authors: Ayanda I. Zulu, Ogunyemi O. Oderinlo, Cuan Kruger, Michelle Isaacs, Heinrich C. Hoppe, Vincent J. Smith, Clinton G. L. Veale, Setshaba D. Khanye
• Format: Article
• Language: English
• Published: MDPI AG 2020-04-01
• Series: Molecules
• Subjects: arylpyrrole; chalcones; trypanosomiasis; <i>Trypanosoma brucei</i>; molecular hybridization
• Online Access: https://www.mdpi.com/1420-3049/25/7/1668
• ISSN: 1420-3049

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 <i>Trypanosoma brucei brucei</i> 427 strain. Several compounds displayed mostly modest in vitro anti-trypanosomal activity with compounds <b>10e</b> and <b>10h</b> 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.