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RESEARCH PRODUCT
Marine inspired antiplasmodial thiazinoquinones: synthesis, computational studies and electrochemical assays
Antonio Doménech-carbóMarialuisa MennaGerardo Cebrián-torrejónMarco PersicoAnna AielloMarcella GuisoPaolo LucianoDonatella TaramelliM. F. SanasiConcetta ImperatoreSilvia ParapiniCaterina Fattorussosubject
SemiquinoneSynthetic derivativesChemistryGeneral Chemical EngineeringOrganic chemistryBiological activityGeneral ChemistryCytotoxicityElectrochemistryCombinatorial chemistryRedoxQuinonedescription
In the search for new antimalarials, we used the quinone scaffold of marine secondary metabolites as a chemical starting point to synthesize new thiazinoquinone compounds. Most of synthetic derivatives have shown a significant pharmacological activity and some structural requirements, critical for both the antiplasmodial effect and cytotoxicity, have been evidenced. The redox properties of the prepared compounds have been investigated by computational studies and electrochemical assays, which indicated that a higher antiplasmodial activity of some thiazinoquinones is related to their greater ability to form the semiquinone species and strongly interact with free Fe(III)-protoporphyrin IX.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2015-01-01 | RSC Advances |