101080-38-0Relevant articles and documents
Synthesis and kinase inhibitory activity of novel substituted indigoids
Beauchard, Anne,Laborie, Helene,Rouillard, Herve,Lozach, Olivier,Ferandin, Yoan,Guevel, Remy Le,Guguen-Guillouzo, Christiane,Meijer, Laurent,Besson, Thierry,Thiery, Valerie
, p. 6257 - 6263 (2009)
The bis-indole indigoids are a promising protein kinase inhibitor scaffold to be further evaluated against the numerous human diseases that imply abnormal regulation of kinases including neurodegenerative disorders. In an effort to identify new pharmacolo
Methylisoindigo and its bromo-derivatives are selective tyrosine kinase inhibitors, repressing cellular stat3 activity, and target CD133+ cancer stem cells in PDAC
Tegethoff, Jana,Bischoff, Roland,Saleh, Sawsan,Blagojevic, Biljana,Merz, Karl-Heinz,Cheng, Xinlai
, (2017)
Indirubin is an active component of the herbal ingredient 'Danggui Longhui wan', which was used for the treatment of inflammation and chronic myeloid leukemia in China. The recent study showed its derivative methylisoindigo (also known as meisoindigo) preferentially targeting cancer stem cells (CSCs) in interference with AMPK and LKB1, the cellular metabolic sensors. In this study, we screened the effect of meisoindigo on a panel of 300 protein kinases and found that it selectively inhibited Stat3-associated tyrosine kinases and further confirmed its activity in cell based assays. To gain a deeper insight into the structure-activity relationship we produced 7 bromo-derivatives exhausting the accessible positions on the bisindole backbone except for in the 4-position due to the space limitation. We compared their anti-proliferative effects on tumor cells. We found that 6-bromomeisoindigo showed improved toxicity in company with increased Stat3 inhibition. Moreover, we detected that 6-bromomeisoindigo induced apoptosis of 95% of CD133+ pancreatic cancer cells. Considering that CD133 is a common marker highly expressed in a range of CSCs, our results imply the potential application of 6-bromomeisoindigo for the treatment of CSCs in different types of cancers.
A 1 - (phenyl) - 2, 3, 4, 9-tetrahydro -1H-pyrido [3,4-b] indole derivatives thereof in the preparation of the application of the anti-tumor drug (by machine translation)
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Paragraph 0066; 0068, (2016/11/14)
The invention belongs to the technical field of pharmaceutical chemistry, in particular to a kind of 1 - (phenyl) - 2, 3, 4, 9-tetrahydro -1H-pyrido [3,4-b] indole derivatives thereof in the preparation of the application of the anti-tumor drugs. Research display inhibit one or more prostandin receptor activity can be effective for the treatment of hypertension, at least one kind of prostagladin E2 receptor in the blood pressure regulating system RAAS in the course of play a crucial role, we by changing 1 and 8 is the angle of the two groups and the distance to EP3 receptor research, we developed a new high-efficiency of the synthetic route to study a series of derivatives, all of the target compound are all new product, all of the compound through the nuclear magnetic resonance and quality of the identification of the structure. The target compound in the antibacterial, anti-tumor, analgesic, anti-platelet aggregation, the promotion of kidney part of the reabsorption of sodium and water, regulating neurotransmitter release, promote adipose tissue Lipolysis and has an important role of anti-arrhythmia. (by machine translation)