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New tricyclic systems as photosensitizers towards triple negative breast cancer cells
Marilia Barreca,Angela Maria Ingarra,Maria Valeria Raimondi,Virginia Spanò,Antonio Palumbo Piccionello,Michele De Franco,Luca Menilli,Valentina Gandin,Giorgia Miolo,Paola Barraja,Alessandra Montalbano 대한약학회 2022 Archives of Pharmacal Research Vol.45 No.11
Nineteen pyrrolo[1,2- h ][1,7]naphthyridinonesand pyrido[2,3- c ]pyrrolo[1,2- a ]azepinones were synthesizedas new tricyclic systems in which the pyridine ringis annelated to the 6,7-dihydroindolizin-8(5 H )-one and5,6,7,8-tetrahydro-9 H -pyrrole[1,2- a ]azepine-9-one moietiesto obtain potential photosensitizing agents. They were testedfor their photoantiproliferative activity on a triple-negativebreast cancer cell line, MDA-MB-231, in the dark and underUVA light (2.0 J/cm 2 ). We demonstrated that their toxicity,only when exposed to light, was primarily due to the generationof reactive oxygen species while their photodegradationproducts were not responsible for their activity. The mostactive compounds exhibited photocytotoxicity with IC 50 valuesat low micromolar level inducing a decrease in the intracellularcontent of thiol, thus triggering cancer cell deaththrough apoptosis. All the pyridone derivatives revealed tobe pure photosensitizers with preferential photocytotoxicactivity towards cancerous over healthy cells. Altogether,the results obtained confi rm pyrrolo[1,2- h ][1,7]naphthyridinonesand pyrido[2,3- c ]pyrrolo[1,2- a ]azepinones as promisingphotosensitisers against triple-negative breast cancer.