The Natural Compound Climacostol as a Prodrug Strategy Based on pH Activation for Efficient Delivery of Cytotoxic Small Agents.

Wittig olefination apoptosis ciliated protists cytotoxic compound pH-activation prodrug strategy small natural agents

Journal

Frontiers in chemistry
ISSN: 2296-2646
Titre abrégé: Front Chem
Pays: Switzerland
ID NLM: 101627988

Informations de publication

Date de publication:
2019
Historique:
received: 11 04 2019
accepted: 11 06 2019
entrez: 19 7 2019
pubmed: 19 7 2019
medline: 19 7 2019
Statut: epublish

Résumé

We synthesized and characterized MOMO as a new small molecule analog of the cytotoxic natural product climacostol efficiently activated in mild extracellular acidosis. The synthesis of MOMO had a key step in the Wittig olefination for the construction of the carbon-carbon double bond in the alkenyl moiety of climacostol. The possibility of obtaining the target (

Identifiants

pubmed: 31316972
doi: 10.3389/fchem.2019.00463
pmc: PMC6609918
doi:

Types de publication

Journal Article

Langues

eng

Pagination

463

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Auteurs

Elisabetta Catalani (E)

Department for Innovation in Biological, Agro-Food and Forest Systems, Università degli Studi della Tuscia, Viterbo, Italy.

Federico Buonanno (F)

Laboratory of Protistology and Biology Education, Department of Education, Cultural Heritage and Tourism, Università degli Studi di Macerata, Macerata, Italy.

Gabriele Lupidi (G)

School of Sciences and Technologies, Section of Chemistry, Università degli Studi di Camerino, Camerino, Italy.

Silvia Bongiorni (S)

Department of Ecological and Biological Sciences, Università degli Studi della Tuscia, Viterbo, Italy.

Riccardo Belardi (R)

Department for Innovation in Biological, Agro-Food and Forest Systems, Università degli Studi della Tuscia, Viterbo, Italy.

Silvia Zecchini (S)

Department of Biomedical and Clinical Sciences "Luigi Sacco" (DIBIC), Università degli Studi di Milano, Milan, Italy.

Matteo Giovarelli (M)

Department of Biomedical and Clinical Sciences "Luigi Sacco" (DIBIC), Università degli Studi di Milano, Milan, Italy.

Marco Coazzoli (M)

Department of Biomedical and Clinical Sciences "Luigi Sacco" (DIBIC), Università degli Studi di Milano, Milan, Italy.

Clara De Palma (C)

Unit of Clinical Pharmacology, University Hospital "Luigi Sacco"-ASST Fatebenefratelli Sacco, Milan, Italy.

Cristiana Perrotta (C)

Department of Biomedical and Clinical Sciences "Luigi Sacco" (DIBIC), Università degli Studi di Milano, Milan, Italy.

Emilio Clementi (E)

Department of Biomedical and Clinical Sciences "Luigi Sacco" (DIBIC), Università degli Studi di Milano, Milan, Italy.
Scientific Institute IRCCS "Eugenio Medea", Bosisio Parini, Italy.

Giorgio Prantera (G)

Department of Ecological and Biological Sciences, Università degli Studi della Tuscia, Viterbo, Italy.

Enrico Marcantoni (E)

School of Sciences and Technologies, Section of Chemistry, Università degli Studi di Camerino, Camerino, Italy.

Claudio Ortenzi (C)

Laboratory of Protistology and Biology Education, Department of Education, Cultural Heritage and Tourism, Università degli Studi di Macerata, Macerata, Italy.

Anna Maria Fausto (AM)

Department for Innovation in Biological, Agro-Food and Forest Systems, Università degli Studi della Tuscia, Viterbo, Italy.

Simona Picchietti (S)

Department for Innovation in Biological, Agro-Food and Forest Systems, Università degli Studi della Tuscia, Viterbo, Italy.

Davide Cervia (D)

Department for Innovation in Biological, Agro-Food and Forest Systems, Università degli Studi della Tuscia, Viterbo, Italy.

Classifications MeSH