0000000000419114

AUTHOR

Simona Di Martino

showing 3 related works from this author

Synthesis of thiazolo[5,4-b]pyridine and [1,3]thiazolo[5,4-h][1,6]naphthyridin-8-one derivatives as potential m-TOR inhibitors

2014

m-TOR inhibitors
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Synthesis and photocytotoxic activity of [1,2,3]triazolo[4,5-h][1,6]naphthyridines and [1,3]oxazolo[5,4-h][1,6]naphthyridines

2018

Abstract [1,2,3]Triazolo[4,5-h][1,6]naphthyridines and [1,3]oxazolo[5,4-h][1,6]naphthyridines were synthesized with the aim to investigate their photocytotoxic activity. Upon irradiation, oxazolo-naphtapyridines induced light-dependent cell death at nanomolar/low micromolar concentrations (EC50 0.01–6.59 μM). The most photocytotoxic derivative showed very high selectivity and photocytotoxicity indexes (SI = 72–86, PTI>5000), along with a triplet excited state with exceptionally long lifetime (18.0 μs) and high molar absorptivity (29781 ± 180 M−1cm−1 at λmax 315 nm). The light-induced production of ROS promptly induced an unquenchable apoptotic process selectively in tumor cells, with mitoch…

Pharmaceutical ScienceApoptosisMitochondrionPhotochemiotherapy; Photosensitizing agents; Reactive oxygen species; [123]Triazolo[45-h][16]naphthyridines; [13]oxazolo[54-h][16]naphthyridines; Pharmacology; Drug Discovery; Pharmaceutical Science; Organic Chemistry01 natural sciencesMedicinal chemistry[13]oxazolo[54-h][16]naphthyridinechemistry.chemical_compoundDrug Discovery6]naphthyridineschemistry.chemical_classification0303 health sciencesTumorPhotosensitizing AgentsCell DeathSinglet OxygenSinglet oxygenPhotochemiotherapy; Photosensitizing agents; Reactive oxygen species; [1; 2; 3]Triazolo[4; 5-h][1; 6]naphthyridines; [1; 3]oxazolo[5; 4-h][1; 6]naphthyridines; Apoptosis; Cell Death; Cell Line; Tumor; Humans; Lysosomes; Mitochondria; Naphthyridines; Photochemotherapy; Photosensitizing Agents; Reactive Oxygen Species; Singlet OxygenGeneral MedicineLysosomeMitochondriaExcited stateReactive oxygen specie5-h][1HumanProgrammed cell death2NaphthyridinePhotochemiotherapy3]Triazolo[4Cell Line03 medical and health sciences4-h][1Cell Line TumorHumansNaphthyridines030304 developmental biologyPharmacologyReactive oxygen speciesPhotosensitizing agent010405 organic chemistryOrganic ChemistryApoptosi0104 chemical sciences3]oxazolo[5chemistryPhotochemotherapyCell cultureApoptosis[123]Triazolo[45-h][16]naphthyridine[1LysosomesReactive Oxygen SpeciesDerivative (chemistry)
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SYNTHESIS OF THIAZOLO[5,4-B]PYRIDINE AND [1,3]THIAZOLO[5,4-H][1,6]NAPHTHYRIDIN-8-ONE DERIVATIVES AS POTENTIAL M-TOR INHIBITORS

2014

M-TOR INHIBITORS
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