Tinto, Francesco
(2017)
Design and chemical synthesis of heterocyclic alkaloid compounds isolated from marine organisms.
[Tesi di dottorato]
| Tipologia del documento: |
Tesi di dottorato
|
| Lingua: |
English |
| Titolo: |
Design and chemical synthesis of heterocyclic alkaloid compounds isolated from marine organisms |
| Autori: |
| Autore | Email |
|---|
| Tinto, Francesco | francescotinto88@gmail.com |
|
| Data: |
9 Aprile 2017 |
| Numero di pagine: |
134 |
| Istituzione: |
Università degli Studi di Napoli Federico II |
| Dipartimento: |
Scienze Chimiche |
| Dottorato: |
Scienze chimiche |
| Ciclo di dottorato: |
29 |
| Coordinatore del Corso di dottorato: |
| nome | email |
|---|
| Paduano, Luigi | lpaduano@unina.it |
|
| Tutor: |
| nome | email |
|---|
| De Castro, Cristina | [non definito] | | Manzo, Emiliano | [non definito] |
|
| Data: |
9 Aprile 2017 |
| Numero di pagine: |
134 |
| Parole chiave: |
Alkaloids; parazoanthines; synthesis; heterocyclic; receptor; hydantoin; guanidine; CXCR4; cancer; HIV-1; pharmacology; chemistry; marine organisms; chemical synthesis; CXCL12; heterocyclic alkaloid; molecular docking; antagonist; CXCR4 antagonist |
| Settori scientifico-disciplinari del MIUR: |
Area 03 - Scienze chimiche > CHIM/06 - Chimica organica |
[error in script]
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| Depositato il: |
03 Mag 2017 17:21 |
| Ultima modifica: |
14 Mar 2018 10:07 |
| URI: |
http://www.fedoa.unina.it/id/eprint/11673 |
| DOI: |
10.6093/UNINA/FEDOA/11673 |
Abstract
Alkaloids are naturally occurring nitrogen containing biologically active heterocyclic compounds. Over the last years, a large number of biologically alkaloids with antiviral, antibacterial, anti-inflammatory, antimalarial, antioxidant and anticancer activities have been isolated from marine source.
In this frame parazoanthines are a group of unique naturally-occurring marine alkaloids reported to date only from the Mediterranean sea anemone Parazoanthus axinellae. The chemical framework characteristic of these molecules is a 3,5-alkyl disubstituted hydantoin core bearing a terminal guanidine and an aromatic ring. Hydantoins and derivatives have been widely used in biomedical studies including novel therapeutic agents of interest as anti-convulsants and antimuscarinics,antiulcers and antiarrythmics, antivirals, antidiabetics, and inhibitors of antagonist of serotonin and fibrinogen receptors, inhibitors of glycine binding site of the NMDA receptor and antagonists of leukocyte cell adhesion.
Due to the biological potential of this class of molecules, a synthetic strategy was planed and developed to prepare natural and not natural analogs of parazoanthines; the molecular docking tests have described a promising antagonist activity on co-chemokine receptor CXCR4, involved in many tumors (breast cancer, melanoma, leukemia multiple myeloma, small cell lung cancer (SCLC), malignant melanoma and pancreatic cancer), rheumatoid arthritis, stem cell mobilization and HIV-1.
The preliminary tests in vitro have confirmed the antagonist effect of parazoanthine-A with the co-receptor CXCR4, describing a promising pharmacological action for the treatment of diseases involved by the activation of this receptor.
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