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

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

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…

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