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

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 cultu...

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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

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spelling	doaj-5632225a6c31411b952e7c68a3807e432020-11-25T02:37:38ZengMDPI AGMolecules1420-30492020-04-01251668166810.3390/molecules25071668Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone DerivativesAyanda I. Zulu0Ogunyemi O. Oderinlo1Cuan Kruger2Michelle Isaacs3Heinrich C. Hoppe4Vincent J. Smith5Clinton G. L. Veale6Setshaba D. Khanye7Department of Chemistry, Faculty of Science, Rhodes University, Grahamstown 6140, South AfricaDepartment of Chemistry, Faculty of Science, Rhodes University, Grahamstown 6140, South AfricaDepartment of Chemistry, Faculty of Science, Rhodes University, Grahamstown 6140, South AfricaCentre for Chemico and Biomedicinal Research, Rhodes University, Grahamstown 6140, South AfricaCentre for Chemico and Biomedicinal Research, Rhodes University, Grahamstown 6140, South AfricaDepartment of Chemistry, Faculty of Science, Rhodes University, Grahamstown 6140, South AfricaSchool of Chemistry and Physics, Pietermaritzburg Campus, University of KwaZulu-Natal, Private Bag X01, Scottsville 3209, South AfricaDepartment of Chemistry, Faculty of Science, Rhodes University, Grahamstown 6140, South AfricaWith 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 IC<sub>50</sub> 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.https://www.mdpi.com/1420-3049/25/7/1668arylpyrrolechalconestrypanosomiasis<i>Trypanosoma brucei</i>molecular hybridization
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Ayanda I. Zulu Ogunyemi O. Oderinlo Cuan Kruger Michelle Isaacs Heinrich C. Hoppe Vincent J. Smith Clinton G. L. Veale Setshaba D. Khanye
spellingShingle	Ayanda I. Zulu Ogunyemi O. Oderinlo Cuan Kruger Michelle Isaacs Heinrich C. Hoppe Vincent J. Smith Clinton G. L. Veale Setshaba D. Khanye Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives Molecules arylpyrrole chalcones trypanosomiasis <i>Trypanosoma brucei</i> molecular hybridization
author_facet	Ayanda I. Zulu Ogunyemi O. Oderinlo Cuan Kruger Michelle Isaacs Heinrich C. Hoppe Vincent J. Smith Clinton G. L. Veale Setshaba D. Khanye
author_sort	Ayanda I. Zulu
title	Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives
title_short	Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives
title_full	Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives
title_fullStr	Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives
title_full_unstemmed	Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives
title_sort	synthesis, structure and in vitro anti-trypanosomal activity of non-toxic arylpyrrole-based chalcone derivatives
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2020-04-01
description	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 IC<sub>50</sub> 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.
topic	arylpyrrole chalcones trypanosomiasis <i>Trypanosoma brucei</i> molecular hybridization
url	https://www.mdpi.com/1420-3049/25/7/1668
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Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives

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