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Antibiotics 2019, 8(1), 9; https://doi.org/10.3390/antibiotics8010009

New Chloramphenicol Derivatives from the Viewpoint of Anticancer and Antimicrobial Activity

1
Department of Biochemistry, School of Medicine, University of Patras, GR-26504 Patras, Greece
2
Laboratory of Synthetic Organic Chemistry, Department of Chemistry, University of Patras, GR-26504 Patras, Greece
3
Laboratory of Public Health, School of Medicine, University of Patras, 26504 Patras, Greece
4
Department of Biochemistry & Biotechnology, University of Thessaly, Biopolis, GR-41500 Larissa, Greece
*
Authors to whom correspondence should be addressed.
Dedicated in memory of the late Prof. Dimitrios L. Kalpaxis.
Received: 19 December 2018 / Revised: 21 January 2019 / Accepted: 23 January 2019 / Published: 29 January 2019
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Abstract

Over the last years, we have been focused on chloramphenicol conjugates that combine in their structure chloramphenicol base with natural polyamines, spermine, spermidine and putrescine, and their modifications. Conjugate 3, with spermidine (SPD) as a natural polyamine linked to chloramphenicol base, showed the best antibacterial and anticancer properties. Using 3 as a prototype, we here explored the influence of the antibacterial and anticancer activity of additional benzyl groups on N1 amino moiety together with modifications of the alkyl length of the aminobutyl fragment of SPD. Our data demonstrate that the novel modifications did not further improve the antibacterial activity of the prototype. However, one of the novel conjugates (4) showed anticancer activity without affecting bacterial growth, thus emerging as a promising anticancer agent, with no adverse effects on bacterial microflora when taken orally. View Full-Text
Keywords: Chloramphenicol; polyamines; conjugates; mitochondrial ribosome; molecular dynamics simulations; antimicrobial activity; anticancer activity; protein biosynthesis; antibiotics Chloramphenicol; polyamines; conjugates; mitochondrial ribosome; molecular dynamics simulations; antimicrobial activity; anticancer activity; protein biosynthesis; antibiotics
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Giannopoulou, P.C.; Missiri, D.A.; Kournoutou, G.G.; Sazakli, E.; Papadopoulos, G.E.; Papaioannou, D.; Dinos, G.P.; Athanassopoulos, C.M.; Kalpaxis, D.L. New Chloramphenicol Derivatives from the Viewpoint of Anticancer and Antimicrobial Activity. Antibiotics 2019, 8, 9.

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