55052-27-2Relevant articles and documents
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.
Preparation method of drug composition for treating febrile convulsion in children
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Paragraph 0017; 0018; 0022-0025, (2019/01/08)
The invention relates to a preparation method of a drug composition for treating febrile convulsion in children. The method comprises a route as shown in the specification. A treatment mechanism of the drug of the invention is to prolong the convulsion latency of a febrile convulsion patient, shorten the convulsion duration, relieve the convulsion seriousness, inhibit apoptosis of hippocampal neurons, regulate the levels of GABA and Glu, relieve the cerebral injury of febrile convulsion patient and finally achieve the purpose of treating the febrile convulsion.
Synthetic method of 6-chloro-7-azaindole
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Paragraph 0046; 0047; 0048, (2017/01/02)
The invention discloses a synthetic method of 6-chloro-7-azaindole, belonging to the field of chemical synthesis. 7-azaindole is taken as a raw material, and the 6-chloro-7-azaindole is synthesized by three actions of N-oxidation, chlorination and hydrolysis. The process route is optimized, and the yield is improved by 70% or more, and is improved by 7% compared with the prior art. The improved synthetic route is simple to operate and feasible, the economic benefits are effectively improved, and large-scale industrial promotion is facilitated.