Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR

Anticancer activity of pyrimidodiazepines based on 2-chloro-4-anilinoquinazoline: synthesis, DNA binding and molecular docking

“…Pyrimidodiazepines are an important bicyclic system due to their biological activities, 17,18 being a very interesting scaffold in medicinal chemistry, which has been incorporated into many drugs as antitumor 19 and antiviral agents, 20,21 given its ability to mimic the nitrogenous bases of nucleic acids. 17,20 Furthermore, pyrimidodiazepines have shown important activity as Aurora A/B, 22 EGFR, 23 and c-Met kinase 19 inhibitors. Fig.…”

An Efficient Synthetic Approach Towards Benzo[b]pyrano[2,3-e][1,4]diazepines, and Their Cytotoxic Activity

“…Compound 15 (IR) showed interest bands centered at 2217 and 3406 cm −1 , owing to the hydroxyl and the nitrile groups, correspondingly, while, its 1 H NMR scope exhibited three new singlets at 3.02, 3.81, and 5.74 ppm, owing to the hydroxyl, methylene, and the secondary amine protons, respectively. In a similar manner, compound 5 was subjected to some selected secondary amines namely; diethylamine, morpholine, N-methylpiperazine and/or piperazinyl to furnish the corresponding tertiary amines (17)(18)(19)(20). Strong absorption sign centered around 2210 cm −1 owing to the nitrile group, supported these structures.…”

“…Found: C,58.12;H,4.74;N,pyrano [2,3-e] [1,4]diazepine-3-carbonitrile (16). White powder (EtOH) with an 80% yield; mp 232-234 17;H,4.12;N,16.37%. Found: C,70.01;H,4.02;N,pyrano [2,3-e] [1,4] ,5.63;N,17.38%.…”

“…1,4-Benzodiazepines ( Figure 1 ) are used as anti-microbial [ 5 ], in alcohol withdrawal syndrome (AWS) [ 6 ], as endothelin antagonist [ 7 ], hypnotics [ 8 ], anxiolytics [ 9 ], anticonvulsants [ 10 ], muscle relaxants [ 10 ], anticancer drugs [ 11 , 12 ], sedatives [ 13 , 14 ], and antipsychotics [ 15 ]. Recently, benzodiazepines were also recognized to have anti-proliferative [ 16 ], antimicrobial [ 17 ], anti-inflammatory [ 18 ], anti-plateletanti-ulcer [ 19 ], and analgesic [ 20 ].…”

Crystal structure of ethyl (E)-1-(3-ethoxy-3-oxoprop-1-en-1-yl)-2-(4-nitrophenyl)-2,5-dihydro-1H-benzo[b][1,4]diazepine-3-carboxylate, C23H23N3O6

“…Benzo[b] [1,4]diazepines are important nitrogen-containing heterocyclic compounds, which have extensive applications in synthetic chemistry [4][5][6] and medicinal chemistry [7][8][9][10]. The crystal structure of title compound is shown in the figure.…”