Research Groups‎ > ‎

BIOMEDCHEM (CHIM/08)

Head of Laboratory: SECCI Daniela 
Sito web:

 

Main Topics:

- Separation by stereo selective HPLC of biologically active chiral molecules.
- Design, synthesis and biological evaluation of new compounds active on Helicobacter pylori, on Candida strains and on other antimicrobial agents.
- Design, synthesis and biological evaluation of new selective inhibitors of monoamine oxidase, MAO-A and MAO-B
- Design, synthesis and biological evaluation of new epigenetic modulators.
- Design, synthesis and biological evaluation of new selective inhibitors of IX and isoforms XII of carbonic anhydrase for the treatment of tumoral pathologies.
- Development and characterization of Monoclonal Antibodies for therapeutic use.


National and International Collaborations:

Dip. di ScienzeFarmacobiologiche, Universita` di Catanzaro “Magna Græcia”
Laboratorio di Chemioterapia Sperimentale - IFO, Roma
Dipartimento di Farmacia, ‘G. D’Annunzio’ Università Chieti
Department of Pharmacology, Fatih, Istanbul
Dipartimento Neurofarba, Università Firenze
Falcudade de Ciencias, Universidade do Porto
Department of Clinical & Experimental Medicine, University of Surrey
Medicinal Chemistry Research Group, Universitè Catholique de Louvain
Facultad de Farmacia, Universidade Santiago de Compostela
Pharmaceutical Chemistry and Centre of Excellence Pharmaceutical Sciences, School of Pharmacy, North-West University, South Africa
Stanley Division of Developmental Neurovirology, Johns Hopkins University School of Medicine,
Baltimora

Facilities:

Rigaku MiniFlex 600 X-ray diffractometer (XRD), Akta Pure 25 M, 1UV-VIS Spectrophotometer
Buchi Rotavapor, Trans Blot Turbo BIO-RAD, Mini Proteam Tetra system Bio-RAD
Power Back Basic BIO-RAD, pH Meter edge/Orp Hanna, Microwave Biotage
Vortex V-1 Plus, Digital Ultrasonic Cleaner, Mini Rocker shaker
Easy Load Masterflex, 
Mark™ MicroplateAbsorbance Reader Bio-Rad 

Settori ERC del gruppo:

PE5 Material and Synthesis
LS7_3 - Pharmacology, pharmacogenomics, drug discovery and design, drug therapy
PE5_17 - Organic chemistry
PE5_16 (Biological chemistry)
PE4_5 (Analytical chemistry)

Grants: (2015-2018)

2015: Progetto Ricerca Universitario, Università di Roma La Sapienza: NON CLASSICAL AND SELECTIVE INHIBITORS OF HUMAN CARBONIC ANHYDRASE ISOFORMS WITH AN INNOVATIVE MECHANISM OF ACTION
2014-2016: POR FESR LAZIO 2007-2013 AVVISO PUBBLICO “INSIEME X VINCERE” PROGETTO R&D FBBV - Farmaci Biosimilari da Biotecnologie Vegetali ricerca promosso da Lazio Innova con partnership del Dipartimento di CTF Università di Roma insieme con l'azienda farmaceutica Special Product's Line
2016: Grandi progetti di Ateneo per la ricerca "New strategies for carbonic anhydrases inhibition: probenecid-amino acidic derivatives as atypical and selective inhibitors of hCA tumor-related isoforms IX and XII".
2018: POR FESR Lazio 2014 - 2020. Progetto T0002E0001 - A0112. Avviso Pubblico "LIFE 2020" - DE n. G.08726/2016. Progetti Integrati "Idonei finanziabili".
2018: Finanziamento delle attività base di ricerca (FABR)

Laboratory Members:

Bizzarri Bruna (R)
Chimenti Paola (AP)
Granese Arianna (R)
Guglielmi Paolo (PhD Student)
Rotondi Giulia

Publication 2015-2018

1. Carradori, S., Secci, D., Petzer, J.P.. MAO inhibitors and their wider applications: a patent review, (2018), Expert Opinion on Therapeutic Patents, 28, 3, pp 211-226.

2. Bellusci, M., Guglielmi, P., Masi, A., Padella, F., Singh, G., Yaacoub, N., Peddis, D., Secci, D.. Magnetic Metal-Organic Framework Composite by Fast and Facile Mechanochemical Process, (2018), Inorganic Chemistry, 57, 4, pp. 1806-1814.

3. Mocan, A., Carradori, S., Locatelli, M., Secci, D., Cesa, S., Mollica, A., Riga, S., Angeli, A., Supuran, C.T., Celia, C., Di Marzio, L., Bioactive isoflavones from Pueraria lobata root and starch: Different extraction techniques and carbonic anhydrase inhibition, (2018), Food and Chemical Toxicology, 112, pp.441-447.

4. Menghini, L., Bellagamba, G., Marcelli, F., De Luca E., Armellani, L., Cifelli, R., Granese, A., Kucukerkan, N., Z., Aktumsek, A., Zengin, G. Analytical Procedures for Secondary Metabolites Determination: Recent Trends and Future Perspectives, (2018), Letters in Drug Design and Discovery, 15(3): pp.281 - 293

5. Carradori, S., Secci, D., Faggi, C., Cirilli, R., A chromatographic study on the exceptional chiral recognition of 2-(benzylsulfinyl)benzamide by an immobilized-type chiral stationary phase based on cellulose tris(3,5-dichlorophenylcarbamate), (2018), Journal of Chromatography A, 1531, pp.151-156.

6. Carradori, S., Ortuso, F., Petzer, A., Bagetta, D., De Monte, C., Secci, D., De Vita, D., Guglielmi, P., Zengin, G., Aktumsek, A., Alcaro, S., Petzer, J.P., Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents, (2018), European Journal of Medicinal Chemistry, 143, pp. 1543-1552.

7. D'Ascenzio, M., Guglielmi, P., Carradori, S., Secci, D., Florio, R., Mollica, A., Ceruso, M., Akdemir, A., Sobolev, A.P., Supuran, C.T. Open saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms (2017) Journal of enzyme inhibition and medicinal chemistry, 32 (1), pp. 51-59. 

8. Nescatelli, R., Carradori, S., Marini, F., Caponigro, V., Bucci, R., De Monte, C., Mollica, A., Mannina, L.,Ceruso, M., Supuran, C.T., Secci,D. Geographical characterization by MAE-HPLC and NIR methodologies and carbonic anhydrase inhibition of Saffron components (2017) Food Chemistry, 221, pp. 855-863.

9. Carradori, S., Bizzarri, B., D'Ascenzio, M., De Monte, C., Grande, R., Rivanera, D., Zicari, A., Mari, E., Sabatino, M., Patsilinakos, A., Ragno, R., Secci, D. Synthesis, biological evaluation and quantitative structure-active relationships of 1,3-thiazolidin-4-one derivatives. A promising chemical scaffold endowed with high antifungal potency and low cytotoxicity (2017) European Journal of Medicinal Chemistry, 140, pp. 274-292.

10. Ferrante, C., Recinella, L., Locatelli, M., Guglielmi, P., Secci, D., Leporini, L., Chiavaroli, A., Leone, S., Martinotti, S., Brunetti, L., Vacca, M., Menghini, L., Orlando, G.Protective Effects Induced by Microwave-Assisted Aqueous Harpagophytum Extract on Rat Cortex Synaptosomes Challenged with Amyloid β-Peptide (2017) Phytotherapy Research, 31 (8), pp. 1257-1264

11. Locatelli, M., Ferrante, C., Carradori, S., Secci, D., Leporini, L., Chiavaroli, A., Leone, S., Recinella, L., Orlando, G., Martinotti, S., Brunetti, L., Vacca, M., Menghini, L.Optimization of Aqueous Extraction and Biological Activity of Harpagophytum procumbens Root on Ex Vivo Rat Colon Inflammatory Model (2017) Phytotherapy Research, 31 (6), pp. 937-944.

12. Pierini, M., Carradori, S., Menta, S., Secci, D., Cirilli, R. 3-(Phenyl-4-oxy)-5-phenyl-4,5-dihydro-(1H)-pyrazole: A fascinating molecular framework to study the enantioseparation ability of the amylose (3,5-dimethyl phenylcarbamate) chiral stationary phase. Part II. Solvophobic effects in enantiorecognition process (2017) Journal of Chromatography A, 1499, pp. 140-148.

13. Carradori, S., Secci, D., Bizzarri, B., Chimenti, P., De Monte, C., Guglielmi, P., Campestre, C., Rivanera, D., Bordón, C., Jones-Brando, L. Synthesis and biological evaluation of anti-Toxoplasma gondii activity of a novel scaffold of thiazolidinone derivatives (2017) Journal of Enzyme Inhibition and Medicinal Chemistry, 32 (1), pp. 746-758.

14. Rinaldi, F., Hanieh, P.N., Longhi, C., Carradori, S., Secci, D., Zengin, G., Ammendolia, M.G., Mattia, E., Del Favero, E., Marianecci, C., Carafa, M. Neem oil nanoemulsions: characterisation and antioxidant activity (2017) Journal of Enzyme Inhibition and Medicinal Chemistry, 32 (1), pp. 1265-1273.

15. Gidaro, M.C., Alcaro, S.,Secci, D., Rivanera, D., Mollica, A., Agamennone, M., Giampietro, L., Carradori, S. Identification of new anti-Candida compounds by ligand-based pharmacophore virtual screening (2016) Journal of Enzyme Inhibition and Medicinal Chemistry, 31 (6), pp. 1703-1706.

16. D’Ascenzio, M., Guglielmi, P., Carradori, S., Secci, D., Florio, R., Mollica, A., Ceruso, M., Akdemir, A., Sobolev, A.P., Supuran, C.T. Open saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms (2016) Journal of Enzyme Inhibition and Medicinal Chemistry, pp. 1-9.

17. Carradori, S., Pierini, M., Menta, S., Secci, D., Fioravanti, R., Cirilli, R. 3-(Phenyl-4-oxy)-5-phenyl-4,5-dihydro-(1H)-pyrazole: A fascinating molecular framework to study the enantioseparation ability of the amylose (3,5-dimethylphenylcarbamate) chiral stationary phase. Part I. Structure-enantioselectivity relationships (2016) Journal of Chromatography A, 1467, pp. 221-227.

18. Secci, D., Carradori, S., Bizzarri, B., Chimenti, P., De Monte, C., Mollica, A., Rivanera, D., Zicari, A., Mari, E., Zengin, G., Aktumsek, A. Novel 1,3-thiazolidin-4-one derivatives as promising anti- Candida agents endowed with anti-oxidant and chelating properties (2016) European Journal of Medicinal Chemistry, 117, pp. 144-156.

19. Carradori, S., Secci, D., De Monte, C., Mollica, A., Ceruso, M., Akdemir, A., Sobolev, A.P., Codispoti, R., De Cosmi, F., Guglielmi, P., Supuran, C.T. A novel library of saccharin and acesulfame derivatives as potent and selective inhibitors of carbonic anhydrase IX and XII isoforms (2016) Bioorganic and Medicinal Chemistry, 24 (5), pp. 1095-1105.

20 .Menta, S., Carradori, S., Siani, G., Secci, D., Mannina, L., Sobolev, A.P., Cirilli, R., Pierini, M. Elucidation of the mechanisms governing the thermal diastereomerization of bioactive chiral 1,3,4-thiadiazoline spiro-cyclohexyl derivatives towards their anancomeric stereoisomers (2016) RSC Advances, 6 (75), pp. 71262-71272.

21. De Monte, C., Carradori, S., Bizzarri, B., Bolasco, A., Caprara, F., Mollica, A., Rivanera, D., Mari, E., Zicari, A., Akdemir, A., Secci, D. Anti-Candida activity and cytotoxicity of a large library of new N-substituted-1,3-thiazolidin-4-one derivatives (2016) European Journal of Medicinal Chemistry, 107, pp. 82-96.

22. Carradori, S., Gidaro,M. C., Petzer, A., Costa,P., Chimenti,P., Alcaro, S.,Petzer,J.P. Inhibition of Human Monoamine Oxidase: Biological and Molecular Modeling Studies on Selected Natural Flavonoids (2016), J. Agric. Food Chem., 64 (47), pp. 9004–9011

23. Carradori, S., Chimenti, P., Fazzari, M., Granese, A., Angiolella, L.Antimicrobial activity, synergism and inhibition of germ tube formation by Crocus sativus-derived compounds against Candida spp (2016), J Enzyme Inhib Med Chem.31 (sup2): pp189-193.

24. Di Martile, M., Desideri, M., De Luca, T., Gabellini, C., Buglioni, S., Eramo, A., Sette, G., Milella, M., Rotili, D., Mai, A., Carradori, S., Secci, D., De Maria, R., Del Bufalo, D., Trisciuoglio, D. Histone acetyltransferase inhibitor CPTH6 preferentially targets lung cancer stem-like cells (2016) Oncotarget, 7 (10), pp. 11332-11348.

25. Menta, S., Carradori, S., Secci, D., Faggi, C., Mannina, L., Cirilli, R., Pierini, M. The Anancomeric Character of the Pharmacophore 1,3,4-Thiadiazoline Framework in Chiral Spiro-Cyclohexyl Derivatives: Effects on Stereochemistry and Spiro-Junction Lability. Thermodynamic Aspects (2015) Journal of Organic Chemistry, 80 (24), pp. 11932-11940.

26. Carradori, S., Mollica, A., Ceruso, M., D’ascenzio, M., De Monte, C., Chimenti, P., Sabia, R., Akdemir, A., Supuran C. T. New amide derivatives of Probenecid as selective inhibitors of carbonic anhydrase IX and XII: biological evaluation and molecular modelling studies (2015), Bioorg. Med. Chem., 23, pp. 2975-2981.

27 .De Monte, C., Carradori, S., Secci, D., D'Ascenzio, M., Guglielmi, P., Mollica, A., Morrone, S., Scarpa, S., Aglianò, A.M., Giantulli, S., Silvestri, I. Synthesis and pharmacological screening of a large library of 1,3,4-thiadiazolines as innovative therapeutic tools for the treatment of prostate cancer and melanoma (2015) European Journal of Medicinal Chemistry, 105, pp. 245-262.

28. D’ascenzio, M., Chimenti, P., Gidaro, M. C., De Monte, C., De Vita, D., Granese, A., Scipione, L., Di Santo, R., Costa, G., Alcaro, S., Yáñez, M., Carradori S. (Thiazol-2-yl)hydrazone derivatives from acetylpyridines as dual inhibitors of MAO and AChE: synthesis, biological evaluation and molecular modeling studies (2015), J. Enzyme Inhib. Med. Chem., 30, pp.908-919.

29. De Monte, C., Bizzarri, B., Gidaro, M. C., Carradori, S., Mollica, A., Luisi, G., Granese, A.,Alcaro, S., Costa, G., Basilico, N. Bioactive compounds of Crocus sativus L. and their semi-synthetic derivatives as promising anti Helicobacter pylori, anti-malarial and anti-leishmanial agents. (2015), Journal of Enzyme Inhibition and Medicinal Chemistry, 30(6), pp.1027-1033

30. D'Ambrosio, K., Carradori, S., Monti, S.M., Buonanno, M., Secci, D., Vullo, D., Supuran, C.T., De Simone, G. Out of the active site binding pocket for carbonic anhydrase inhibitors (2015) Chemical Communications, 51 (2), pp. 302-305.

31. Carradori, S., Mollica, A., De Monte, C., Granese, A., Supuran, C. T. Nitric oxide donors and selective carbonic anhydrase inhibitors: a dual pharmacological approach for the treatment of glaucoma, cancer and osteoporosis (2015) Molecules, 20, pp.5667-5679.

32. Carradori, S., Mannina, L., De Cosmi, F., Beccarini, T., Secci, D., Sobolev, A.P.
Optimization of the microwave-assisted extraction of azadirachta indica (Neem) leaves using NMR-based metabolic fingerprinting (2015) Current Bioactive Compounds, 11 (3), pp. 142-145.