288148-80-1

Basic information

• Product Name: 9-nitropyrido[2,3-b][1,5]benzoxazepin-5(6H)-one
• Synonyms: 9-nitropyrido[2,3-b][1,5]benzoxazepin-5(6H)-one
• CAS NO: 288148-80-1
• Molecular Formula: C₁₂H₇N₃O₄
• Molecular Weight: 257.20168
• Mol File: 288148-80-1.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 9-nitropyrido[2,3-b][1,5]benzoxazepin-5(6H)-one(CAS DataBase Reference)
• NIST Chemistry Reference: 9-nitropyrido[2,3-b][1,5]benzoxazepin-5(6H)-one(288148-80-1)
• EPA Substance Registry System: 9-nitropyrido[2,3-b][1,5]benzoxazepin-5(6H)-one(288148-80-1)

Safety Data

• Hazardous Substances Data: 288148-80-1(Hazardous Substances Data)

Upstream product

• 288148-78-7 2-chloro-N-(2-hydroxy-4-nitro-phenyl)nicotinamide 
• 121-88-0 5-Nitro-2-aminophenol 
• 49609-84-9 2-Chloronicotinoyl chloride 
• 609-71-2 2-hydroxy-3-carboxypyridine 
• 2942-59-8 2-chloronicotinic acid 

Downstream Products

• 140413-13-4 10-Methyl-7-nitro-10H-5-oxa-4,10-diaza-dibenzo[a,d]cyclohepten-11-one 
• 140413-14-5 7-Amino-10-methyl-10H-5-oxa-4,10-diaza-dibenzo[a,d]cyclohepten-11-one 

Relevant articles and documents

Pyrido[2,3-b][1,5]benzoxazepin-5(6H)-one derivatives as CDK8 inhibitors

CDK8 is a cyclin-dependent kinase that forms part of the mediator complex, and modulates the transcriptional output from distinct transcription factors involved in oncogenic control. Overexpression of CDK8 has been observed in various cancers, representing a potential target for developing novel CDK8 inhibitors in cancer therapeutics. In the course of our investigations to discover new CDK8 inhibitors, we designed and synthesized tricyclic pyrido[2,3-b][1,5]benzoxazepin-5(6H)-one derivatives, by introduction of chemical complexity in the multi-kinase inhibitor Sorafenib taking into account the flexibility of the P-loop motif of CDK8 protein observed after analysis of structural information of co-crystallized CDK8 inhibitors. In vitro evaluation of the inhibitory activity of the prepared compounds against CDK8 led us to identify compound 2 as the most potent inhibitor of the series (IC50 = 8.25 nM). Co-crystal studies and the remarkable selectivity profile of compound 2 are presented. Compound 2 showed moderate reduction of phosphorylation of CDK8 substrate STAT1 in cells, in line with other reported Type II CDK8 inhibitors. We propose herein an alternative to find a potential therapeutic use for this chemical series.

Hepatitis C viral IRES inhibition by phenazine and phenazine-like molecules

An in vitro assay based on the expression of Fluci reporter gene under the translational control of HCV IRES was used to evaluate and screen compound libraries. A structure-activity relationship study on a phenazine hit was conducted. Our data suggest that an intact phenazine or phenazine-like core with two distal polar substitutions is crucial for potency. (C) 2000 Elsevier Science Ltd. All rights reserved.

Novel Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase. 2. Tricyclic Pyridobenzoxazepinones and Dibenzoxazepinones

Dibenzoxazepin-11(10H)-ones (III), pyridobenzoxazepin-6(5H)-ones (IV), and pyridobenzoxazepin-5(6H)-ones (V) were found to inhibit human immunodeficiency virus type 1 reverse transcriptase with IC50 values as 19 nM.A-ring substitution has a profound effect on activity, with appropriate substituents at the positions ortho and para to the lactam nitrogen providing dramatically enhanced potency.Substitution in the C-ring is generally neutral or detrimental to activity.Although a C-ring amino substituent at the position meta to the lactam carbonyl is generally beneficial to activity, it has essentially no effect when the A-ring is optimally substituted.Like the dipyridodiazepinone nevirapine, compounds III-V are specific for HIV-1 RT, exhibiting no inhibitory activity against HIV-2 RT or other virial reverse transcriptase enzymes.