Zobi, Fabio

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orcid::0000-0002-9077-7184
  • Zobi, Fabio (7)
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Author's Bibliography

Efficient Direct Nitrosylation of alpha-Diimine Rhenium Tricarbonyl Complexes to Structurally Nearly Identical Higher Charge Congeners Activable towards Photo-CO Release

Sovari, Sara Nasiri; Kolly, Isabelle; Schindler, Kevin; Cortat, Youri; Liu, Shing-Chi; Crochet, Aurelien; Pavić, Aleksandar; Zobi, Fabio

(MDPI, Basel, 2021)

TY  - JOUR
AU  - Sovari, Sara Nasiri
AU  - Kolly, Isabelle
AU  - Schindler, Kevin
AU  - Cortat, Youri
AU  - Liu, Shing-Chi
AU  - Crochet, Aurelien
AU  - Pavić, Aleksandar
AU  - Zobi, Fabio
PY  - 2021
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1459
AB  - The reaction of rhenium alpha-diimine (N-N) tricarbonyl complexes with nitrosonium tetrafluoroborate yields the corresponding dicarbonyl-nitrosyl [Re(CO)(2)(NO)(N-N)X](+) species (where X = halide). The complexes, accessible in a single step in good yield, are structurally nearly identical higher charge congeners of the tricarbonyl molecules. Substitution chemistry aimed at the realization of equivalent dicationic species (intended for applications as potential antimicrobial agents), revealed that the reactivity of metal ion in [Re(CO)(2)(NO)(N-N)X](+) is that of a hard Re acid, probably due to the stronger pi-acceptor properties of NO+ as compared to those of CO. The metal ion thus shows great affinity for pi-basic ligands, which are consequently difficult to replace by, e.g., sigma-donor or weak pi-acids like pyridine. Attempts of direct nitrosylation of alpha-diimine fac-[Re(CO)(3)](+) complexes bearing pi-basic OR-type ligands gave the [Re(CO)(2)(NO)(N-N)(BF4)][BF4] salt as the only product in good yield, featuring a stable Re-FBF3 bond. The solid state crystal structure of nearly all molecules presented could be elucidated. A fundamental consequence of the chemistry of [Re(CO)(2)(NO)(N-N)X](+) complexes, it that the same can be photo-activated towards CO release and represent an entirely new class of photoCORMs.
PB  - MDPI, Basel
T2  - Molecules
T1  - Efficient Direct Nitrosylation of alpha-Diimine Rhenium Tricarbonyl Complexes to Structurally Nearly Identical Higher Charge Congeners Activable towards Photo-CO Release
IS  - 17
VL  - 26
DO  - 10.3390/molecules26175302
ER  - 
@article{
author = "Sovari, Sara Nasiri and Kolly, Isabelle and Schindler, Kevin and Cortat, Youri and Liu, Shing-Chi and Crochet, Aurelien and Pavić, Aleksandar and Zobi, Fabio",
year = "2021",
abstract = "The reaction of rhenium alpha-diimine (N-N) tricarbonyl complexes with nitrosonium tetrafluoroborate yields the corresponding dicarbonyl-nitrosyl [Re(CO)(2)(NO)(N-N)X](+) species (where X = halide). The complexes, accessible in a single step in good yield, are structurally nearly identical higher charge congeners of the tricarbonyl molecules. Substitution chemistry aimed at the realization of equivalent dicationic species (intended for applications as potential antimicrobial agents), revealed that the reactivity of metal ion in [Re(CO)(2)(NO)(N-N)X](+) is that of a hard Re acid, probably due to the stronger pi-acceptor properties of NO+ as compared to those of CO. The metal ion thus shows great affinity for pi-basic ligands, which are consequently difficult to replace by, e.g., sigma-donor or weak pi-acids like pyridine. Attempts of direct nitrosylation of alpha-diimine fac-[Re(CO)(3)](+) complexes bearing pi-basic OR-type ligands gave the [Re(CO)(2)(NO)(N-N)(BF4)][BF4] salt as the only product in good yield, featuring a stable Re-FBF3 bond. The solid state crystal structure of nearly all molecules presented could be elucidated. A fundamental consequence of the chemistry of [Re(CO)(2)(NO)(N-N)X](+) complexes, it that the same can be photo-activated towards CO release and represent an entirely new class of photoCORMs.",
publisher = "MDPI, Basel",
journal = "Molecules",
title = "Efficient Direct Nitrosylation of alpha-Diimine Rhenium Tricarbonyl Complexes to Structurally Nearly Identical Higher Charge Congeners Activable towards Photo-CO Release",
number = "17",
volume = "26",
doi = "10.3390/molecules26175302"
}
Sovari, S. N., Kolly, I., Schindler, K., Cortat, Y., Liu, S., Crochet, A., Pavić, A.,& Zobi, F.. (2021). Efficient Direct Nitrosylation of alpha-Diimine Rhenium Tricarbonyl Complexes to Structurally Nearly Identical Higher Charge Congeners Activable towards Photo-CO Release. in Molecules
MDPI, Basel., 26(17).
https://doi.org/10.3390/molecules26175302
Sovari SN, Kolly I, Schindler K, Cortat Y, Liu S, Crochet A, Pavić A, Zobi F. Efficient Direct Nitrosylation of alpha-Diimine Rhenium Tricarbonyl Complexes to Structurally Nearly Identical Higher Charge Congeners Activable towards Photo-CO Release. in Molecules. 2021;26(17).
doi:10.3390/molecules26175302 .
Sovari, Sara Nasiri, Kolly, Isabelle, Schindler, Kevin, Cortat, Youri, Liu, Shing-Chi, Crochet, Aurelien, Pavić, Aleksandar, Zobi, Fabio, "Efficient Direct Nitrosylation of alpha-Diimine Rhenium Tricarbonyl Complexes to Structurally Nearly Identical Higher Charge Congeners Activable towards Photo-CO Release" in Molecules, 26, no. 17 (2021),
https://doi.org/10.3390/molecules26175302 . .
3
3

Combatting AMR: A molecular approach to the discovery of potent and non-toxic rhenium complexes active against C. albicans-MRSA co-infection

Sovari, Sara Nasiri; Radaković, Nataša; Roch, Paul; Crochet, Aurelien; Pavić, Aleksandar; Zobi, Fabio

(Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux, 2021)

TY  - JOUR
AU  - Sovari, Sara Nasiri
AU  - Radaković, Nataša
AU  - Roch, Paul
AU  - Crochet, Aurelien
AU  - Pavić, Aleksandar
AU  - Zobi, Fabio
PY  - 2021
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1477
AB  - Antimicrobial resistance (AMR) is a major emerging threat to public health, causing serious issues in the successful prevention and treatment of persistent diseases. While the problem escalates, lack of financial incentive has lead major pharmaceutical companies to interrupt their antibiotic drug discovery programs. The World Health Organisation (WHO) has called for novel solutions outside the traditional development pathway, with emphasis on new classes of active compounds with non-classical mechanisms of action. Metal complexes are an untapped source of antibiotic potential owing to unique modes of action and a wider range of three-dimensional geometries as compared to purely organic compounds. In this study, we present the antimicrobial and antifungal efficacy of a family of rhenium tricarbonyl diimine complexes with varying ligands, charge and lipophilicity. Our study allowed the identification of potent and non-toxic complexes active in vivo against S. aureus infections at MIC doses as low as 300 ng/mL, as well as against C. albicans-MRSA mixed co-infection. The compounds are capable of suppressing the C. albicans morphogenetic yeast-to-hyphal transition, eradicating fungal-S. aureus co-infection, while showing no sign of cardio-, hepato-, hematotoxiciy or teratogenicity.
PB  - Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux
T2  - European Journal of Medicinal Chemistry
T1  - Combatting AMR: A molecular approach to the discovery of potent and non-toxic rhenium complexes active against C. albicans-MRSA co-infection
VL  - 226
DO  - 10.1016/j.ejmech.2021.113858
ER  - 
@article{
author = "Sovari, Sara Nasiri and Radaković, Nataša and Roch, Paul and Crochet, Aurelien and Pavić, Aleksandar and Zobi, Fabio",
year = "2021",
abstract = "Antimicrobial resistance (AMR) is a major emerging threat to public health, causing serious issues in the successful prevention and treatment of persistent diseases. While the problem escalates, lack of financial incentive has lead major pharmaceutical companies to interrupt their antibiotic drug discovery programs. The World Health Organisation (WHO) has called for novel solutions outside the traditional development pathway, with emphasis on new classes of active compounds with non-classical mechanisms of action. Metal complexes are an untapped source of antibiotic potential owing to unique modes of action and a wider range of three-dimensional geometries as compared to purely organic compounds. In this study, we present the antimicrobial and antifungal efficacy of a family of rhenium tricarbonyl diimine complexes with varying ligands, charge and lipophilicity. Our study allowed the identification of potent and non-toxic complexes active in vivo against S. aureus infections at MIC doses as low as 300 ng/mL, as well as against C. albicans-MRSA mixed co-infection. The compounds are capable of suppressing the C. albicans morphogenetic yeast-to-hyphal transition, eradicating fungal-S. aureus co-infection, while showing no sign of cardio-, hepato-, hematotoxiciy or teratogenicity.",
publisher = "Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux",
journal = "European Journal of Medicinal Chemistry",
title = "Combatting AMR: A molecular approach to the discovery of potent and non-toxic rhenium complexes active against C. albicans-MRSA co-infection",
volume = "226",
doi = "10.1016/j.ejmech.2021.113858"
}
Sovari, S. N., Radaković, N., Roch, P., Crochet, A., Pavić, A.,& Zobi, F.. (2021). Combatting AMR: A molecular approach to the discovery of potent and non-toxic rhenium complexes active against C. albicans-MRSA co-infection. in European Journal of Medicinal Chemistry
Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux., 226.
https://doi.org/10.1016/j.ejmech.2021.113858
Sovari SN, Radaković N, Roch P, Crochet A, Pavić A, Zobi F. Combatting AMR: A molecular approach to the discovery of potent and non-toxic rhenium complexes active against C. albicans-MRSA co-infection. in European Journal of Medicinal Chemistry. 2021;226.
doi:10.1016/j.ejmech.2021.113858 .
Sovari, Sara Nasiri, Radaković, Nataša, Roch, Paul, Crochet, Aurelien, Pavić, Aleksandar, Zobi, Fabio, "Combatting AMR: A molecular approach to the discovery of potent and non-toxic rhenium complexes active against C. albicans-MRSA co-infection" in European Journal of Medicinal Chemistry, 226 (2021),
https://doi.org/10.1016/j.ejmech.2021.113858 . .
3
29
1
24

Neovascularization Effects of Carbon Monoxide Releasing Drugs Chemisorbed on Coscinodiscus Diatoms Carriers Characterized by Spectromicroscopy Imaging

Delasoie, Joachim; Radaković, Nataša; Pavić, Aleksandar; Zobi, Fabio

(MDPI, Basel, 2020)

TY  - JOUR
AU  - Delasoie, Joachim
AU  - Radaković, Nataša
AU  - Pavić, Aleksandar
AU  - Zobi, Fabio
PY  - 2020
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1335
AB  - Silica microparticles made of diatomaceous earth have become particularly attractive materials for designing drug delivery systems. In order to investigate the use of natural diatoms as drug scaffolds for carbon monoxide releasing molecules (CORMs), we evaluated the chemisorption of the cis-[Re(CO)(2)Br-4](2-) complex (ReCORM-2) and its vitamin B-12 derivative (B-12-ReCORM-2) on Coscinodiscus frustules by 3D FT-IR spectroscopic imaging, and the drugs' neovascularization effects in vivo in the zebrafish (Danio rerio) model. By mapping the symmetric Re-C equivalent to O upsilon(CO) stretching vibration of the CORMs in the 2000 cm(-1) region, we found that the drugs are mostly localized at the girdle band of the diatom frustule. Both ReCORM-2 and B-12-ReCORM-2 retain their CO-releasing ability when chemisorbed on the diatoms. When applied in vivo at doses  gt = 25 mu M, the molecules markedly reduced intersegmental and subintestinal vessels development in zebrafish, revealing high anti-angiogenic potential. In addition, diatom frustules did not provoke any toxic in vivo response in the zebrafish embryos, including inflammation. Overall, our results indicate that: (1) CORMs chemisorbed on diatom frustules retain their CO-releasing abilities; (2) both CO-releasing molecules show a concentration-dependent effect on the neovascularization in developing zebrafish; (3) silicate frustules are not toxic and could be used as CORMs drug carriers.
PB  - MDPI, Basel
T2  - Applied Sciences-Basel
T1  - Neovascularization Effects of Carbon Monoxide Releasing Drugs Chemisorbed on Coscinodiscus Diatoms Carriers Characterized by Spectromicroscopy Imaging
IS  - 20
VL  - 10
DO  - 10.3390/app10207380
ER  - 
@article{
author = "Delasoie, Joachim and Radaković, Nataša and Pavić, Aleksandar and Zobi, Fabio",
year = "2020",
abstract = "Silica microparticles made of diatomaceous earth have become particularly attractive materials for designing drug delivery systems. In order to investigate the use of natural diatoms as drug scaffolds for carbon monoxide releasing molecules (CORMs), we evaluated the chemisorption of the cis-[Re(CO)(2)Br-4](2-) complex (ReCORM-2) and its vitamin B-12 derivative (B-12-ReCORM-2) on Coscinodiscus frustules by 3D FT-IR spectroscopic imaging, and the drugs' neovascularization effects in vivo in the zebrafish (Danio rerio) model. By mapping the symmetric Re-C equivalent to O upsilon(CO) stretching vibration of the CORMs in the 2000 cm(-1) region, we found that the drugs are mostly localized at the girdle band of the diatom frustule. Both ReCORM-2 and B-12-ReCORM-2 retain their CO-releasing ability when chemisorbed on the diatoms. When applied in vivo at doses  gt = 25 mu M, the molecules markedly reduced intersegmental and subintestinal vessels development in zebrafish, revealing high anti-angiogenic potential. In addition, diatom frustules did not provoke any toxic in vivo response in the zebrafish embryos, including inflammation. Overall, our results indicate that: (1) CORMs chemisorbed on diatom frustules retain their CO-releasing abilities; (2) both CO-releasing molecules show a concentration-dependent effect on the neovascularization in developing zebrafish; (3) silicate frustules are not toxic and could be used as CORMs drug carriers.",
publisher = "MDPI, Basel",
journal = "Applied Sciences-Basel",
title = "Neovascularization Effects of Carbon Monoxide Releasing Drugs Chemisorbed on Coscinodiscus Diatoms Carriers Characterized by Spectromicroscopy Imaging",
number = "20",
volume = "10",
doi = "10.3390/app10207380"
}
Delasoie, J., Radaković, N., Pavić, A.,& Zobi, F.. (2020). Neovascularization Effects of Carbon Monoxide Releasing Drugs Chemisorbed on Coscinodiscus Diatoms Carriers Characterized by Spectromicroscopy Imaging. in Applied Sciences-Basel
MDPI, Basel., 10(20).
https://doi.org/10.3390/app10207380
Delasoie J, Radaković N, Pavić A, Zobi F. Neovascularization Effects of Carbon Monoxide Releasing Drugs Chemisorbed on Coscinodiscus Diatoms Carriers Characterized by Spectromicroscopy Imaging. in Applied Sciences-Basel. 2020;10(20).
doi:10.3390/app10207380 .
Delasoie, Joachim, Radaković, Nataša, Pavić, Aleksandar, Zobi, Fabio, "Neovascularization Effects of Carbon Monoxide Releasing Drugs Chemisorbed on Coscinodiscus Diatoms Carriers Characterized by Spectromicroscopy Imaging" in Applied Sciences-Basel, 10, no. 20 (2020),
https://doi.org/10.3390/app10207380 . .
6
6

Design, synthesis and in vivo evaluation of 3-arylcoumarin derivatives of rhenium(I) tricarbonyl complexes as potent antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA)

Sovari, Sara Nasiri; Vojnović, Sandra; Škaro Bogojević, Sanja; Crochet, Aurelien; Pavić, Aleksandar; Nikodinović-Runić, Jasmina; Zobi, Fabio

(Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux, 2020)

TY  - JOUR
AU  - Sovari, Sara Nasiri
AU  - Vojnović, Sandra
AU  - Škaro Bogojević, Sanja
AU  - Crochet, Aurelien
AU  - Pavić, Aleksandar
AU  - Nikodinović-Runić, Jasmina
AU  - Zobi, Fabio
PY  - 2020
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1365
AB  - We have prepared a series of ten 3-arylcoumarin molecules, their respective fac-[Re(CO)(3)(bpy)L](+) and fac-[Re(CO)(3)(L(sic)L)Br] complexes and tested all compounds for their antimicrobial efficacy. Whereas the 3-arylcoumarin ligands are virtually inactive against the human-associated pathogens with minimum inhibitory concentrations (MICs)  gt  150 mu M, when coordinated to the fac-[Re(CO)(3)](+) core, most of the resulting complexes showed remarkable antibacterial potency. Several rhenium complexes exhibit activity in nanomolar concentrations against Gram-positive pathogens such as Staphylococcus aureus strains, including methicillin-resistant S. aureus (MRSA) and Enterococcus faecium. The molecules do not affect bacterial cell membrane potential, but some of the most potent complexes strongly interact with DNA, indicating it as a possible target for their mode of action. In vivo studies in the zebrafish model showed that the complexes with anti-staphylococcal/MRSA activity were non-toxic to the organism even at much higher doses of the corresponding MICs. In the zebrafish-MRSA infection model, the complexes increased the survival rate of infected fish up to 100% and markedly reduced bacterial burden. Moreover, all rescued fish developed normally following the treatments with the metallic compounds.
PB  - Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux
T2  - European Journal of Medicinal Chemistry
T1  - Design, synthesis and in vivo evaluation of 3-arylcoumarin derivatives of rhenium(I) tricarbonyl complexes as potent antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA)
VL  - 205
DO  - 10.1016/j.ejmech.2020.112533
ER  - 
@article{
author = "Sovari, Sara Nasiri and Vojnović, Sandra and Škaro Bogojević, Sanja and Crochet, Aurelien and Pavić, Aleksandar and Nikodinović-Runić, Jasmina and Zobi, Fabio",
year = "2020",
abstract = "We have prepared a series of ten 3-arylcoumarin molecules, their respective fac-[Re(CO)(3)(bpy)L](+) and fac-[Re(CO)(3)(L(sic)L)Br] complexes and tested all compounds for their antimicrobial efficacy. Whereas the 3-arylcoumarin ligands are virtually inactive against the human-associated pathogens with minimum inhibitory concentrations (MICs)  gt  150 mu M, when coordinated to the fac-[Re(CO)(3)](+) core, most of the resulting complexes showed remarkable antibacterial potency. Several rhenium complexes exhibit activity in nanomolar concentrations against Gram-positive pathogens such as Staphylococcus aureus strains, including methicillin-resistant S. aureus (MRSA) and Enterococcus faecium. The molecules do not affect bacterial cell membrane potential, but some of the most potent complexes strongly interact with DNA, indicating it as a possible target for their mode of action. In vivo studies in the zebrafish model showed that the complexes with anti-staphylococcal/MRSA activity were non-toxic to the organism even at much higher doses of the corresponding MICs. In the zebrafish-MRSA infection model, the complexes increased the survival rate of infected fish up to 100% and markedly reduced bacterial burden. Moreover, all rescued fish developed normally following the treatments with the metallic compounds.",
publisher = "Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux",
journal = "European Journal of Medicinal Chemistry",
title = "Design, synthesis and in vivo evaluation of 3-arylcoumarin derivatives of rhenium(I) tricarbonyl complexes as potent antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA)",
volume = "205",
doi = "10.1016/j.ejmech.2020.112533"
}
Sovari, S. N., Vojnović, S., Škaro Bogojević, S., Crochet, A., Pavić, A., Nikodinović-Runić, J.,& Zobi, F.. (2020). Design, synthesis and in vivo evaluation of 3-arylcoumarin derivatives of rhenium(I) tricarbonyl complexes as potent antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA). in European Journal of Medicinal Chemistry
Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux., 205.
https://doi.org/10.1016/j.ejmech.2020.112533
Sovari SN, Vojnović S, Škaro Bogojević S, Crochet A, Pavić A, Nikodinović-Runić J, Zobi F. Design, synthesis and in vivo evaluation of 3-arylcoumarin derivatives of rhenium(I) tricarbonyl complexes as potent antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA). in European Journal of Medicinal Chemistry. 2020;205.
doi:10.1016/j.ejmech.2020.112533 .
Sovari, Sara Nasiri, Vojnović, Sandra, Škaro Bogojević, Sanja, Crochet, Aurelien, Pavić, Aleksandar, Nikodinović-Runić, Jasmina, Zobi, Fabio, "Design, synthesis and in vivo evaluation of 3-arylcoumarin derivatives of rhenium(I) tricarbonyl complexes as potent antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA)" in European Journal of Medicinal Chemistry, 205 (2020),
https://doi.org/10.1016/j.ejmech.2020.112533 . .
1
49
1
50

Identification of novel potent and non-toxic anticancer, anti-angiogenic and antimetastatic rhenium complexes against colorectal carcinoma

Delasoie, Joachim; Pavić, Aleksandar; Voutier, Noemie; Vojnović, Sandra; Crochet, Aurelien; Nikodinović-Runić, Jasmina; Zobi, Fabio

(Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux, 2020)

TY  - JOUR
AU  - Delasoie, Joachim
AU  - Pavić, Aleksandar
AU  - Voutier, Noemie
AU  - Vojnović, Sandra
AU  - Crochet, Aurelien
AU  - Nikodinović-Runić, Jasmina
AU  - Zobi, Fabio
PY  - 2020
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1360
AB  - Combination therapy targeting both tumor growth and vascularization is considered to be a cornerstone for colorectal carcinomas (CRC) treatment. However, the major obstacles of most clinical anticancer drugs are their weak selective activity towards cancer cells and inherent inner organs toxicity, accompanied with fast drug resistance development. In our effort to discover novel selective and non-toxic agents effective against CRC, we designed, synthesized and characterized a series of rhenium(I) tricarbonyl-based complexes with increased lipophilicity. Two of these novel compounds were discovered to possess remarkable anticancer, anti-angiogenic and antimetastatic activity in vivo (zebrafish-human HCT-116 xenograft model), being effective at very low doses (1-3 mu M). At doses as high as 250 mu M the complexes did not provoke toxicity issues encountered in clinical anticancer drugs (cardio-, hepato-, and myelotoxicity). In vivo assays showed that the two compounds exceed the anti-tumor and anti-angiogenic activity of clinical drugs cisplatin and sunitinib malate, and display a large therapeutic window.
PB  - Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux
T2  - European Journal of Medicinal Chemistry
T1  - Identification of novel potent and non-toxic anticancer, anti-angiogenic and antimetastatic rhenium complexes against colorectal carcinoma
VL  - 204
DO  - 10.1016/j.ejmech.2020.112583
ER  - 
@article{
author = "Delasoie, Joachim and Pavić, Aleksandar and Voutier, Noemie and Vojnović, Sandra and Crochet, Aurelien and Nikodinović-Runić, Jasmina and Zobi, Fabio",
year = "2020",
abstract = "Combination therapy targeting both tumor growth and vascularization is considered to be a cornerstone for colorectal carcinomas (CRC) treatment. However, the major obstacles of most clinical anticancer drugs are their weak selective activity towards cancer cells and inherent inner organs toxicity, accompanied with fast drug resistance development. In our effort to discover novel selective and non-toxic agents effective against CRC, we designed, synthesized and characterized a series of rhenium(I) tricarbonyl-based complexes with increased lipophilicity. Two of these novel compounds were discovered to possess remarkable anticancer, anti-angiogenic and antimetastatic activity in vivo (zebrafish-human HCT-116 xenograft model), being effective at very low doses (1-3 mu M). At doses as high as 250 mu M the complexes did not provoke toxicity issues encountered in clinical anticancer drugs (cardio-, hepato-, and myelotoxicity). In vivo assays showed that the two compounds exceed the anti-tumor and anti-angiogenic activity of clinical drugs cisplatin and sunitinib malate, and display a large therapeutic window.",
publisher = "Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux",
journal = "European Journal of Medicinal Chemistry",
title = "Identification of novel potent and non-toxic anticancer, anti-angiogenic and antimetastatic rhenium complexes against colorectal carcinoma",
volume = "204",
doi = "10.1016/j.ejmech.2020.112583"
}
Delasoie, J., Pavić, A., Voutier, N., Vojnović, S., Crochet, A., Nikodinović-Runić, J.,& Zobi, F.. (2020). Identification of novel potent and non-toxic anticancer, anti-angiogenic and antimetastatic rhenium complexes against colorectal carcinoma. in European Journal of Medicinal Chemistry
Elsevier France-Editions Scientifiques Medicales Elsevier, Issy-Les-Moulineaux., 204.
https://doi.org/10.1016/j.ejmech.2020.112583
Delasoie J, Pavić A, Voutier N, Vojnović S, Crochet A, Nikodinović-Runić J, Zobi F. Identification of novel potent and non-toxic anticancer, anti-angiogenic and antimetastatic rhenium complexes against colorectal carcinoma. in European Journal of Medicinal Chemistry. 2020;204.
doi:10.1016/j.ejmech.2020.112583 .
Delasoie, Joachim, Pavić, Aleksandar, Voutier, Noemie, Vojnović, Sandra, Crochet, Aurelien, Nikodinović-Runić, Jasmina, Zobi, Fabio, "Identification of novel potent and non-toxic anticancer, anti-angiogenic and antimetastatic rhenium complexes against colorectal carcinoma" in European Journal of Medicinal Chemistry, 204 (2020),
https://doi.org/10.1016/j.ejmech.2020.112583 . .
1
49
1
44

Photoactivatable Surface-Functionalized Diatom Microalgae for Colorectal Cancer Targeted Delivery and Enhanced Cytotoxicity of Anticancer Complexes

Delasoie, Joachim; Schiel, Philippe; Vojnović, Sandra; Nikodinović-Runić, Jasmina; Zobi, Fabio

(MDPI, Basel, 2020)

TY  - JOUR
AU  - Delasoie, Joachim
AU  - Schiel, Philippe
AU  - Vojnović, Sandra
AU  - Nikodinović-Runić, Jasmina
AU  - Zobi, Fabio
PY  - 2020
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1301
AB  - Systemic toxicity and severe side effects are commonly associated with anticancer chemotherapies. New strategies based on enhanced drug selectivity and targeted delivery to cancer cells while leaving healthy tissue undamaged can reduce the global patient burden. Herein, we report the design, synthesis and characterization of a bio-inspired hybrid multifunctional drug delivery system based on diatom microalgae. The microalgae's surface was chemically functionalized with hybrid vitamin B-12-photoactivatable molecules and the materials further loaded with highly active rhenium(I) tricarbonyl anticancer complexes. The constructs showed enhanced adherence to colorectal cancer (CRC) cells and slow release of the chemotherapeutic drugs. The overall toxicity of the hybrid multifunctional drug delivery system was further enhanced by photoactivation of the microalgae surface. Depending on the construct and anticancer drug, a 2-fold increase in the cytotoxic efficacy of the drug was observed upon light irradiation. The use of this targeted drug delivery strategy, together with selective spatial-temporal light activation, may lead to lower effective concentration of anticancer drugs, thereby reducing medication doses, possible side effects and overall burden for the patient.
PB  - MDPI, Basel
T2  - Pharmaceutics
T1  - Photoactivatable Surface-Functionalized Diatom Microalgae for Colorectal Cancer Targeted Delivery and Enhanced Cytotoxicity of Anticancer Complexes
IS  - 5
VL  - 12
DO  - 10.3390/pharmaceutics12050480
ER  - 
@article{
author = "Delasoie, Joachim and Schiel, Philippe and Vojnović, Sandra and Nikodinović-Runić, Jasmina and Zobi, Fabio",
year = "2020",
abstract = "Systemic toxicity and severe side effects are commonly associated with anticancer chemotherapies. New strategies based on enhanced drug selectivity and targeted delivery to cancer cells while leaving healthy tissue undamaged can reduce the global patient burden. Herein, we report the design, synthesis and characterization of a bio-inspired hybrid multifunctional drug delivery system based on diatom microalgae. The microalgae's surface was chemically functionalized with hybrid vitamin B-12-photoactivatable molecules and the materials further loaded with highly active rhenium(I) tricarbonyl anticancer complexes. The constructs showed enhanced adherence to colorectal cancer (CRC) cells and slow release of the chemotherapeutic drugs. The overall toxicity of the hybrid multifunctional drug delivery system was further enhanced by photoactivation of the microalgae surface. Depending on the construct and anticancer drug, a 2-fold increase in the cytotoxic efficacy of the drug was observed upon light irradiation. The use of this targeted drug delivery strategy, together with selective spatial-temporal light activation, may lead to lower effective concentration of anticancer drugs, thereby reducing medication doses, possible side effects and overall burden for the patient.",
publisher = "MDPI, Basel",
journal = "Pharmaceutics",
title = "Photoactivatable Surface-Functionalized Diatom Microalgae for Colorectal Cancer Targeted Delivery and Enhanced Cytotoxicity of Anticancer Complexes",
number = "5",
volume = "12",
doi = "10.3390/pharmaceutics12050480"
}
Delasoie, J., Schiel, P., Vojnović, S., Nikodinović-Runić, J.,& Zobi, F.. (2020). Photoactivatable Surface-Functionalized Diatom Microalgae for Colorectal Cancer Targeted Delivery and Enhanced Cytotoxicity of Anticancer Complexes. in Pharmaceutics
MDPI, Basel., 12(5).
https://doi.org/10.3390/pharmaceutics12050480
Delasoie J, Schiel P, Vojnović S, Nikodinović-Runić J, Zobi F. Photoactivatable Surface-Functionalized Diatom Microalgae for Colorectal Cancer Targeted Delivery and Enhanced Cytotoxicity of Anticancer Complexes. in Pharmaceutics. 2020;12(5).
doi:10.3390/pharmaceutics12050480 .
Delasoie, Joachim, Schiel, Philippe, Vojnović, Sandra, Nikodinović-Runić, Jasmina, Zobi, Fabio, "Photoactivatable Surface-Functionalized Diatom Microalgae for Colorectal Cancer Targeted Delivery and Enhanced Cytotoxicity of Anticancer Complexes" in Pharmaceutics, 12, no. 5 (2020),
https://doi.org/10.3390/pharmaceutics12050480 . .
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Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins

Rossier, Jeremie; Sovari, Sara Nasiri; Pavić, Aleksandar; Vojnović, Sandra; Stringer, Tameryn; Battig, Sarah; Smith, Gregory S.; Nikodinović-Runić, Jasmina; Zobi, Fabio

(MDPI, Basel, 2019)

TY  - JOUR
AU  - Rossier, Jeremie
AU  - Sovari, Sara Nasiri
AU  - Pavić, Aleksandar
AU  - Vojnović, Sandra
AU  - Stringer, Tameryn
AU  - Battig, Sarah
AU  - Smith, Gregory S.
AU  - Nikodinović-Runić, Jasmina
AU  - Zobi, Fabio
PY  - 2019
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1276
AB  - We have explored the possibility of using organometallic derivatives of cobalamin as a scaffold for the delivery of the same antimalarial drug to both erythro- and hepatocytes. This hybrid molecule approach, intended as a possible tool for the development of multi-stage antimalarial agents, pivots on the preparation of azide-functionalized drugs which, after coupling to the vitamin, are released with a 4-(4-ethynylphenyl)-triazole functionality. Three chloroquine and one imidazolopiperazine derivative (based on the KAF156 structure) were selected as model drugs. One hybrid chloroquine conjugate was extensively studied via fluorescent labelling for in vitro and in vivo bio-distribution studies and gave proof-of-concept for the design. It showed no toxicity in vivo (zebrafish model) as well as no hepatotoxicity, no cardiotoxicity or developmental toxicity of the embryos. All 4-(4-ethynylphenyl)-triazole derivatives of chloroquine were equally active against chloroquine-resistant (CQR) and chloroquine-sensitive (CQS) Plasmodium falciparum strains.
PB  - MDPI, Basel
T2  - Molecules
T1  - Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins
IS  - 12
VL  - 24
DO  - 10.3390/molecules24122310
ER  - 
@article{
author = "Rossier, Jeremie and Sovari, Sara Nasiri and Pavić, Aleksandar and Vojnović, Sandra and Stringer, Tameryn and Battig, Sarah and Smith, Gregory S. and Nikodinović-Runić, Jasmina and Zobi, Fabio",
year = "2019",
abstract = "We have explored the possibility of using organometallic derivatives of cobalamin as a scaffold for the delivery of the same antimalarial drug to both erythro- and hepatocytes. This hybrid molecule approach, intended as a possible tool for the development of multi-stage antimalarial agents, pivots on the preparation of azide-functionalized drugs which, after coupling to the vitamin, are released with a 4-(4-ethynylphenyl)-triazole functionality. Three chloroquine and one imidazolopiperazine derivative (based on the KAF156 structure) were selected as model drugs. One hybrid chloroquine conjugate was extensively studied via fluorescent labelling for in vitro and in vivo bio-distribution studies and gave proof-of-concept for the design. It showed no toxicity in vivo (zebrafish model) as well as no hepatotoxicity, no cardiotoxicity or developmental toxicity of the embryos. All 4-(4-ethynylphenyl)-triazole derivatives of chloroquine were equally active against chloroquine-resistant (CQR) and chloroquine-sensitive (CQS) Plasmodium falciparum strains.",
publisher = "MDPI, Basel",
journal = "Molecules",
title = "Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins",
number = "12",
volume = "24",
doi = "10.3390/molecules24122310"
}
Rossier, J., Sovari, S. N., Pavić, A., Vojnović, S., Stringer, T., Battig, S., Smith, G. S., Nikodinović-Runić, J.,& Zobi, F.. (2019). Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins. in Molecules
MDPI, Basel., 24(12).
https://doi.org/10.3390/molecules24122310
Rossier J, Sovari SN, Pavić A, Vojnović S, Stringer T, Battig S, Smith GS, Nikodinović-Runić J, Zobi F. Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins. in Molecules. 2019;24(12).
doi:10.3390/molecules24122310 .
Rossier, Jeremie, Sovari, Sara Nasiri, Pavić, Aleksandar, Vojnović, Sandra, Stringer, Tameryn, Battig, Sarah, Smith, Gregory S., Nikodinović-Runić, Jasmina, Zobi, Fabio, "Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins" in Molecules, 24, no. 12 (2019),
https://doi.org/10.3390/molecules24122310 . .
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