1015609-91-2Relevant academic research and scientific papers
A one-pot three-component synthesis of fused Spiro-Indoline/Indene derivatives derived from ethynyl azaindole by 1,3-dipolar cycloaddition reaction
Narayanarao, Manjunatha,Koodlur, Lokesh,Gopal, Subramanya,Reddy, Suman Y.,Kamila, Susmita
, p. 2441 - 2451 (2018)
A one-pot method for the simple, efficient, and environmentally benign protocol for the synthesis of Spiro-Indoline/Indene derivatives containing Aza indole moiety as a side chain is outlined. The 1,3-dipolar cycloaddition reaction of azomethine ylides derived from ethynyl Azaindole under mild conditions is accomplished. The low cost, easy availability of the starting material, and simple reaction conditions suggest the possible use of the present method for large-scale preparations.
Solution-phase parallel synthesis of ruxolitinib-derived Janus kinase inhibitors via copper-catalyzed azide-alkyne cycloaddition
Gehringer, Matthias,Forster, Michael,Laufer, Stefan A.
, p. 5 - 10 (2015)
A solution-phase parallel synthesis of triazole-derived ruxolitinib analogues was developed in the current study. The method employs copper-catalyzed azide-alkyne cycloaddition to build up the central triazole template. Product isolation by precipitation
Synthesis of novel 7-azaindole derivatives containing pyridin-3-ylmethyl dithiocarbamate moiety as potent PKM2 activators and PKM2 nucleus translocation inhibitors
Liu, Bin,Yuan, Xia,Xu, Bo,Zhang, Han,Li, Ridong,Wang, Xin,Ge, Zemei,Li, Runtao
, p. 1 - 15 (2019/03/17)
Multiple lines of evidence have indicated that pyruvate kinase M2 (PKM2) is upregulated in most cancer cells and it is increasingly recognized as a potential therapeutic target in oncology. In a continuation of our discovery of lead compound 5 and SAR study, the 7-azaindole moiety in compound 5 was systematically optimized. The results showed that compound 6f, which has a difluoroethyl substitution on the 7-azaindole ring, exhibited high PKM2 activation potency and anti-proliferation activities on A375 cell lines. In a xenograft mouse model, oral administration of compound 6f led to significant tumor regression without obvious toxicity. Further mechanistic studies revealed that 6f could influence the translocation of PKM2 into nucleus, as well as induction of apoptosis and autophagy of A375 cells. More importantly, compound 6f significantly inhibited migration of A375 cells in a concentration-dependent manner. Collectively, 6f may serve as a lead compound in the development of potent PKM2 activators for cancer therapy.
PROTEIN KINASE INHIBITORS AND USE THEREOF
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Page/Page column 19, (2011/11/30)
Disclosed are compounds according to Formula I: wherein the variables are described herein.
Multistep synthesis of a new tricyclic azaindole-based scaffold
Angiolini, Mauro,Borgia, Andrea Lombardi,Bandiera, Tiziano
body text, p. 5156 - 5158 (2009/12/05)
In this Letter the synthetic pathway adopted for the preparation of a new functionalized tricyclic scaffold containing the 7-azaindole moiety is presented. An intramolecular palladium-mediated reaction is described as the crucial step for a condensed seve
