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

Risultato della ricerca: Articlepeer review

8 Citazioni (Scopus)


[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 mitochondrial and lysosomal involvement. Altogether, these results demonstrate that the most active compound acts as a promising singlet oxygen sensitizer for biological applications.
Lingua originaleEnglish
pagine (da-a)176-193-193
Numero di pagine18
RivistaEuropean Journal of Medicinal Chemistry
Stato di pubblicazionePublished - 2019

All Science Journal Classification (ASJC) codes

  • ???subjectarea.asjc.3000.3004???
  • ???subjectarea.asjc.3000.3002???
  • ???subjectarea.asjc.1600.1605???


Entra nei temi di ricerca di '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'. Insieme formano una fingerprint unica.

Cita questo