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Article

Anti-Tumoral Effects of a (1H-Pyrrol-1-yl)Methyl-1H-Benzoimidazole Carbamate Ester Derivative on Head and Neck Squamous Carcinoma Cell Lines

1
Department of Experimental Medicine, “Sapienza” University of Rome, Viale Regina Elena 324, 00161 Rome, Italy
2
Department of Sensory Organs, “Sapienza” University of Rome, Viale del Policlinico 155, 00161 Rome, Italy
3
Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, “Sapienza” Università di Roma, P.le Aldo Moro 5, 00185 Rome, Italy
4
Department of Environmental Biology, “Sapienza” University of Rome, p.le Aldo Moro 5, 00185 Rome, Italy
*
Author to whom correspondence should be addressed.
These authors contributed equally to this manuscript.
Academic Editor: Luís M. T. Frija
Pharmaceuticals 2021, 14(6), 564; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14060564
Received: 25 May 2021 / Revised: 8 June 2021 / Accepted: 9 June 2021 / Published: 12 June 2021
(This article belongs to the Special Issue Recent Developments in the Medicinal Chemistry of Pyrroles)
Nocodazole is an antineoplastic agent that exerts its effects by depolymerizing microtubules. Herein we report a structural analog of nocodazole, a (1H-pyrrol-1-yl)methyl-1H-benzoimidazole carbamate ester derivative, named RDS 60. We evaluated the antineoplastic properties of RDS 60 in two human head and neck squamous cell carcinoma (HNSCC) cell lines and we found that this compound significantly inhibited replication of both HNSCC cell lines without inducing any important cytotoxic effect on human dermal fibroblasts and human keratinocytes. The treatment of HNSCC cell lines with 1 μM RDS 60 for 24 h stopped development of normal bipolar mitotic spindles and, at the same time, blocked the cell cycle in G2/M phase together with cytoplasmic accumulation of cyclin B1. Consequently, treatment with 2 μM RDS 60 for 24 h induced the activation of apoptosis in both HNSCC cell lines. Additionally, RDS 60 was able to reverse the epithelial-mesenchymal transition and to inhibit cell migration and extracellular matrix infiltration of both HNSCC cell lines. The reported results demonstrate that this compound has a potent effect in blocking cell cycle, inducing apoptosis and inhibiting cell motility and stromal invasion of HNSCC cell lines. Therefore, the ability of RDS 60 to attenuate the malignancy of tumor cells suggests its potential role as an interesting and powerful tool for new approaches in treating HNSCC. View Full-Text
Keywords: pyrroles; benzimidazoles; nocodazole; head and neck squamous cell carcinoma; apoptosis; epithelial-mesenchymal transition; tubulin pyrroles; benzimidazoles; nocodazole; head and neck squamous cell carcinoma; apoptosis; epithelial-mesenchymal transition; tubulin
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MDPI and ACS Style

Nicolai, A.; Madia, V.N.; Messore, A.; De Vita, D.; De Leo, A.; Ialongo, D.; Tudino, V.; Tortorella, E.; Scipione, L.; Taurone, S.; Pergolizzi, T.; Artico, M.; Di Santo, R.; Costi, R.; Scarpa, S. Anti-Tumoral Effects of a (1H-Pyrrol-1-yl)Methyl-1H-Benzoimidazole Carbamate Ester Derivative on Head and Neck Squamous Carcinoma Cell Lines. Pharmaceuticals 2021, 14, 564. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14060564

AMA Style

Nicolai A, Madia VN, Messore A, De Vita D, De Leo A, Ialongo D, Tudino V, Tortorella E, Scipione L, Taurone S, Pergolizzi T, Artico M, Di Santo R, Costi R, Scarpa S. Anti-Tumoral Effects of a (1H-Pyrrol-1-yl)Methyl-1H-Benzoimidazole Carbamate Ester Derivative on Head and Neck Squamous Carcinoma Cell Lines. Pharmaceuticals. 2021; 14(6):564. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14060564

Chicago/Turabian Style

Nicolai, Alice, Valentina N. Madia, Antonella Messore, Daniela De Vita, Alessandro De Leo, Davide Ialongo, Valeria Tudino, Elisabetta Tortorella, Luigi Scipione, Samanta Taurone, Tiziano Pergolizzi, Marco Artico, Roberto Di Santo, Roberta Costi, and Susanna Scarpa. 2021. "Anti-Tumoral Effects of a (1H-Pyrrol-1-yl)Methyl-1H-Benzoimidazole Carbamate Ester Derivative on Head and Neck Squamous Carcinoma Cell Lines" Pharmaceuticals 14, no. 6: 564. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14060564

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