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Upstream product

• 607-32-9 5-nitroisoquinoline 
• 1127-49-7 5,8-diaminoisoquinoline 
• 156901-61-0 8-amino-5-nitro-isoquinoline 
• 104-94-9 4-methoxy-aniline 
• 84289-03-2 DA 295 

Relevant academic research and scientific papers

Fluorescent 1,4-Naphthoquinones to Visualize Diffuse and Dense-Core Amyloid Plaques in APP/PS1 Transgenic Mouse Brains

Recent clinical approvals of brain imaging radiotracers targeting amyloid-β provided clinicians the tools to detect and confirm Alzheimer's disease pathology without autopsy or biopsy. While current imaging agents are effective in postsymptomatic Alzheimer's patients, there is much room for improvement in earlier diagnosis, hence prompting a need for new and improved amyloid imaging agents. Here we synthesized 41 novel 1,4-naphthoquinone derivatives and initially discovered 14 antiamyloidogenic compounds via in vitro amyloid-β aggregation assay; however, qualitative analyses of these compounds produced conflicting results and required further investigation. Follow-up docking and biophysical studies revealed that four of these compounds penetrate the blood-brain barrier, directly bind to amyloid-β aggregates, and enhance fluorescence properties upon interaction. These compounds specifically stain both diffuse and dense-core amyloid-β plaques in brain sections of APP/PS1 double transgenic Alzheimer's mouse models. Our findings suggest 1,4-naphthoquinones as a new scaffold for amyloid-β imaging agents for early stage Alzheimer's.

Synthesis of 6-chloroisoquinoline-5,8-diones and pyrido[3,4-b]phenazine-5,12-diones and evaluation of their cytotoxicity and DNA topoisomerase II inhibitory activity

The substituted chloroisoquinolinediones and pyrido[3,4-b]phenazinediones were synthesized, and the cytotoxic activity and topoisomerase II inhibitory activity of the prepared compounds were evaluated. Chloroisoquinolinediones have been prepared by the re

7-(Substituted-phenyl)amino-5,8-isoquinolinediones: Synthesis and cytotoxic activities on cancer cell lines

6-Chloro-7-(substituted-phenyl)amino-5,8-isoquinolinediones (3a-3u) and 7-(substituted-phenyl)amino-5,8-isoquinolinediones (4a-4d) were synthesized by nucleophilic substitution of 6,7-dichloro-5,8-isoquinolinedione (8) and 5,8-isoquinolinedione (9) with appropriate arylamines. The quinones 3a-3u and 4a-4d were evaluated for in vitro cytotoxic activities against five solid tumor cell lines such as A549, SK-OV-3, SK-MEL-2, XF498 and HCT-15. Among them, 3c, 3d, 3f and 3h exhibited potent activities against the cell lines HCT-15 and SK-MEL-2.

Synthesis and cytotoxic activities of 6-chloro-7-arylamino-5,8- isoquinolinediones

6-Chloro-7-arylamino-5,8-isoquinolinediones were newly synthesized and evaluated for in vitro cytotoxic activities against five human solid tumor cell lines. Among them, 5b, 5c and 5d exhibited potent activities against the cell lines HCT-15 and SK-MEL-2.