Pyrrolo[3′,2′:6,7]cyclohepta[1,2-b]pyridines with potent photo-antiproliferative activity

New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation

“…In the framework of our research on polycyclic nitrogen systems, [16,17,18,19,20,21,22,23,24,25,26,27,28,29,30,31,32,33] particularly referring to nortopsentin alkaloid analogues [34,35,36,37,38,39], herein we report the synthesis of the new series of thiazoles 1 (Table 1) and their evaluation as antibiofilm agents. In this series of nortopsentin analogues, the imidazole core of the natural product is replaced by the thiazole ring and one of the indole units is replaced by a 7-aza-indole moiety decorated with an ethanamine chain bound to the imine nitrogen.…”

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

“…Phototoxicity was assessed by MTT test 72 h after UV irradiation in the presence of the compounds. [17,18] Phototoxicity was evaluated only for compounds with adequate solubility in DMSO and reported as the effective concentration able to kill 50% of the cell population (EC50 , Table 4); toxicity in the absence of UV exposure was indicated as the cytotoxic concentration able to kill 50% of the cell population (CC50). Oct 7.)…”

“…[16] More recently we have studied pyrrolo [3',2':6,7]cyclohepta [1,2-d]pyrimidines (11) and pyrrolo [3',2':6,7]cyclohepta [1,2-b]pyridines (12) which showed very promising antitumor properties. [17,18] Upon photoactivation with light of the proper wavelength, they showed cytotoxic effect at 0.06-4.96 μM and 0.19-10.70 μM respectively, inducing apoptosis associated with rapid and massive production of large amounts of ROS, mitochondrial morphology modifications and activation of lysosomes. Unfortunately, although these two classes of derivatives were endowed with potent photocytotoxic activity, they were not very selective for tumor cell lines.…”

“…Student T-test (two tailed, P<0.01) was performed and assessed that data obtained for 6e-treated cells were statistically significant, while 5h-treated cells were comparable to control non-treated cells. As compared to other photoactivated compounds, oxazolo-derivatives pushed the majority of cell population into an irreversible apoptotic process in a shorter time lapse [17,18]. The triggering of apoptosis is a favourable feature for a chemotherapic drug, since, unlike necrosis, the apoptotic process does not cause an inflammatory reaction.2.2.7 Cytotoxicity mechanisms: mitochondrial and lysosomal-dependent ROS response Different intracellular signaling pathways, including mitochondrial dysfunction and lysosome activation, trigger and carry on the apoptotic process; we thus proceeded examining both mitochondrial and lysosomal involvement in 6e-treated photoactivated cells.…”

Synthesis of novel pyridine linked to benzimidazole via sulphide and their Antioxident and Antimicrobial activity

“…Imidazo [4, 5-c] pyridine derivatives displayed promising antimicrobial activity 10 . Pyridine derivatives displayed antimicrobial activity .Anti-cancer [17][18][19] , Anti-tumor [20][21][22] , Anti-Psychotic 23 , Anti-proliferative [24][25][26] . Based on the above information, we have identified novel Pyridine derivatives endowed with anti oxidantand antimicrobial activities.…”