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Article

New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents

1
Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, via Archirafi 32, 90123 Palermo, Italy
2
Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, viale delle Scienze, Building 16, 90128 Palermo, Italy
3
Pharmaceutical Department, Provincial Health Authority (ASP) of Palermo, via Pindemonte 88, 90129 Palermo, Italy
*
Authors to whom correspondence should be addressed.
These authors contributed equally to the work.
Received: 7 May 2020 / Revised: 22 May 2020 / Accepted: 28 May 2020 / Published: 30 May 2020
Pyrrolomycins (PMs) are polyhalogenated antibiotics known as powerful biologically active compounds, yet featuring high cytotoxicity. The present study reports the antibacterial and antitumoral properties of new chemically synthesized PMs, where the three positions of the pyrrolic nucleus were replaced by nitro groups, aiming to reduce their cytotoxicity while maintaining or even enhancing the biological activity. Indeed, the presence of the nitro substituent in diverse positions of the pyrrole determined an improvement of the minimal bactericidal concentration (MBC) against Gram-positive (i.e., Staphylococcus aureus) or -negative (i.e., Pseudomonas aeruginosa) pathogen strains as compared to the natural PM-C. Moreover, some new nitro-PMs were as active as or more than PM-C in inhibiting the proliferation of colon (HCT116) and breast (MCF 7) cancer cell lines and were less toxic towards normal epithelial (hTERT RPE-1) cells. Altogether, our findings contribute to increase the knowledge of the mode of action of these promising molecules and provide a basis for their rationale chemical or biological manipulation. View Full-Text
Keywords: heterocycles; pyrrolic nucleus; pyrrolomycin; antibacterial activity; Pseudomonas aeruginosa; Staphylococcus aureus; antitumoral activity; HCT116; MCF 7 heterocycles; pyrrolic nucleus; pyrrolomycin; antibacterial activity; Pseudomonas aeruginosa; Staphylococcus aureus; antitumoral activity; HCT116; MCF 7
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MDPI and ACS Style

Raimondi, M.V.; Presentato, A.; Li Petri, G.; Buttacavoli, M.; Ribaudo, A.; De Caro, V.; Alduina, R.; Cancemi, P. New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents. Antibiotics 2020, 9, 292. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9060292

AMA Style

Raimondi MV, Presentato A, Li Petri G, Buttacavoli M, Ribaudo A, De Caro V, Alduina R, Cancemi P. New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents. Antibiotics. 2020; 9(6):292. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9060292

Chicago/Turabian Style

Raimondi, Maria V., Alessandro Presentato, Giovanna Li Petri, Miriam Buttacavoli, Agnese Ribaudo, Viviana De Caro, Rosa Alduina, and Patrizia Cancemi. 2020. "New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents" Antibiotics 9, no. 6: 292. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9060292

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