Imidazopyridine-fused [1,3]-diazepinones: Synthesis and antiproliferative activity

Nano silica-bonded N-propylsulfamic acid as an efficient and environmentally benign catalyst for the synthesis of 1,5-benzodiazepines

“…With the aim to develop high-performance heterogenized catalyst, herein, we wish to report synthesis of nanosilica-bonded N-propylsulfamic acid (NSBNPSA) and evaluation of its catalytic activity by synthesizing a library of benzodiazepines. It is pertinent to mention that benzodiazepines are privileged scaffolds in heterocyclic chemistry and extensively used as anticancer, antiproliferative, sedative, hypnotic, analgesic, anti-inflammatory, antipyretic, anticonvulsant, antimitotic, antimicrobial, antianxiety, and antidepressive agents [11][12][13][14][15][16][17][18]. The methods available in the literature for its…”

Imidazopyridine-fused [1,3]diazepinones: modulations of positions 2 to 4 and their impacts on the anti-melanoma activity

“…The cell cycle analysis was performed as previously described to compare data with our previous results 10 . Flow cytometric analysis was performed on 350,000 MDA-MB-435 cells seeded in culture dishes (60 mm diameter) and allowed to grow for 48 h. Cells were then treated with compound 5 or 8 at 5 mM concentration for 16 h and 48 h. After treatment cells were harvested and fixed with 70% ethanol.…”

“…To evaluate the effect of compound treatment on cell morphology and stress actin fibres, an immunofluorescence imaging of cells was performed as previously described 10 . MDA-MB-435 cells were seeded on cover slips in petri dishes and allowed to grow for 24 h. After cell growth, cells were treated with the vehicule (control cells) or with JMV5038, compound 5 or 8 at 5 mM for 20 h. Then cells were fixed using Antigenfix for 20 min and permeabilized using 0.2% Triton X-100 for 4 min at room temperature.…”

“…Recently, we reported the discovery of JMV5038, an original pyrido-imidazodiazepinone derivative, using a screening on the NCI-60 cancer cell line panel 10 . This compound showed a promising activity on several cancer cell lines, with a growth inhibition of 50% (GI 50 ) in the low micromolar range on melanoma cells and with no significant cytotoxic activity on NIH-3T3 fibroblasts, even at 100 mM.…”

CuI/I2‐Mediated Intramolecular Oxidative Cyclization Reaction of N‐(2‐pyridyl)amidines by the Direct Double C−H Functionalization of a C(sp3)−H Bond

“…The pharmacological activities of imidazo[1,2‐ a ]‐pyridine derivatives have been shown to be dependent on the nature of the substituents, including their tethered positions. For example, imidazo[1,2‐ a ]‐pyridines with 2‐amino groups on the imidazole ring show a wide range of biological activities, such as antirhinovirus, protein kinase inhibition,and antiproliferative agents (Figure ) . However, a further literature investigation indicated that only a limited number of studies have reported the synthesis of compounds containing a 2‐aminoimidazo[1,2‐ a ]‐pyridine skeleton.…”