Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures

Heterocyclic compounds are one of the main groups of organic compounds possessing wide range of applications in various areas of science and their derivatives are present in many bioactive structures. They display a wide variety of biological activities. Recently, more and more attention has been fo...

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Autores principales:	Benas Balandis, Vytautas Mickevičius, Vilma Petrikaitė
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	benzenesulfonamides imidazoles alkylated anticancer activity colony formation tumor spheroids Medicine R Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/c187c460eecc4fa590622c9bb4483d8c
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spelling	oai:doaj.org-article:c187c460eecc4fa590622c9bb4483d8c2021-11-25T18:39:48ZExploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures10.3390/ph141111581424-8247https://doaj.org/article/c187c460eecc4fa590622c9bb4483d8c2021-11-01T00:00:00Zhttps://www.mdpi.com/1424-8247/14/11/1158https://doaj.org/toc/1424-8247Heterocyclic compounds are one of the main groups of organic compounds possessing wide range of applications in various areas of science and their derivatives are present in many bioactive structures. They display a wide variety of biological activities. Recently, more and more attention has been focused to such heterocyclic compounds as azoles. In this work, we have synthesized a series of new imidazole derivatives incorporating a benzenesulfonamide moiety in their structure, which then were evaluated for their cytotoxicity against human triple-negative breast cancer MDA-MB-231 and human malignant melanoma IGR39 cell lines by MTT assay. Benzenesulfonamide-bearing imidazole derivatives containing 4-chloro and 3,4-dichlorosubstituents in benzene ring, and 2-ethylthio and 3-ethyl groups in imidazole ring have been determined as the most active compounds. Half-maximal effective concentration (EC<sub>50</sub>) of the most cytotoxic compound was 27.8 ± 2.8 µM against IGR39 cell line and 20.5 ± 3.6 µM against MDA-MB-231 cell line. Compounds reduced cell colony formation of both cell lines and inhibited the growth and viability of IGR39 cell spheroids more efficiently compared to triple-negative breast cancer spheroids.Benas BalandisVytautas MickevičiusVilma PetrikaitėMDPI AGarticlebenzenesulfonamidesimidazolesalkylatedanticancer activitycolony formationtumor spheroidsMedicineRPharmacy and materia medicaRS1-441ENPharmaceuticals, Vol 14, Iss 1158, p 1158 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	benzenesulfonamides imidazoles alkylated anticancer activity colony formation tumor spheroids Medicine R Pharmacy and materia medica RS1-441
spellingShingle	benzenesulfonamides imidazoles alkylated anticancer activity colony formation tumor spheroids Medicine R Pharmacy and materia medica RS1-441 Benas Balandis Vytautas Mickevičius Vilma Petrikaitė Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures
description	Heterocyclic compounds are one of the main groups of organic compounds possessing wide range of applications in various areas of science and their derivatives are present in many bioactive structures. They display a wide variety of biological activities. Recently, more and more attention has been focused to such heterocyclic compounds as azoles. In this work, we have synthesized a series of new imidazole derivatives incorporating a benzenesulfonamide moiety in their structure, which then were evaluated for their cytotoxicity against human triple-negative breast cancer MDA-MB-231 and human malignant melanoma IGR39 cell lines by MTT assay. Benzenesulfonamide-bearing imidazole derivatives containing 4-chloro and 3,4-dichlorosubstituents in benzene ring, and 2-ethylthio and 3-ethyl groups in imidazole ring have been determined as the most active compounds. Half-maximal effective concentration (EC<sub>50</sub>) of the most cytotoxic compound was 27.8 ± 2.8 µM against IGR39 cell line and 20.5 ± 3.6 µM against MDA-MB-231 cell line. Compounds reduced cell colony formation of both cell lines and inhibited the growth and viability of IGR39 cell spheroids more efficiently compared to triple-negative breast cancer spheroids.
format	article
author	Benas Balandis Vytautas Mickevičius Vilma Petrikaitė
author_facet	Benas Balandis Vytautas Mickevičius Vilma Petrikaitė
author_sort	Benas Balandis
title	Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures
title_short	Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures
title_full	Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures
title_fullStr	Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures
title_full_unstemmed	Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures
title_sort	exploration of benzenesulfonamide-bearing imidazole derivatives activity in triple-negative breast cancer and melanoma 2d and 3d cell cultures
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/c187c460eecc4fa590622c9bb4483d8c
work_keys_str_mv	AT benasbalandis explorationofbenzenesulfonamidebearingimidazolederivativesactivityintriplenegativebreastcancerandmelanoma2dand3dcellcultures AT vytautasmickevicius explorationofbenzenesulfonamidebearingimidazolederivativesactivityintriplenegativebreastcancerandmelanoma2dand3dcellcultures AT vilmapetrikaite explorationofbenzenesulfonamidebearingimidazolederivativesactivityintriplenegativebreastcancerandmelanoma2dand3dcellcultures
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Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures

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