327600-47-5Relevant academic research and scientific papers
2-AMINOPYRIMIDINE DERIVATIVE, PREPARATION METHOD AND USE THEREOF
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, (2021/03/04)
The disclosure provides an aminopyrimidine derivative for preventing and treating diseases related to IDH mutation, a preparation method and use thereof. Specifically, the disclosure provides a compound of Formula I, a stereoisomer, racemate thereof, or pharmaceutically acceptable salt thereof. The compound of the general Formula I has isocitrate dehydrogenase 1 (IDH1) inhibitory activity and can treat cancer induced by IDH1 mutation.
Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration
Cao, Hengyi,Zhu, Guangya,Sun, Lin,Chen, Ge,Ma, Xinxin,Luo, Xiao,Zhu, Jidong
, (2019/09/30)
Isocitrate dehydrogenase 1 (IDH1), which catalyzes the conversion of isocitrate to α-ketoglutarate, is one of key enzymes in the tricarboxylic acid cycle (TCA). Hotspot mutation at Arg132 in IDH1 that alters the function of IDH1 by further converting the α-ketoglutarate(α-KG) to 2-hydroxyglutarate (2-HG) have been identified in a variety of cancers. Because the IDH1 mutations occur in a significant portion of gliomas and glioblastomas, it is important that IDH1 inhibitors have to be brain penetrant to treat IDH1-mutant brain tumors. Here we report the efforts to design and synthesize a novel serial of mutant IDH1 inhibitors with improved activity and the blood-brain barrier (BBB) penetration. We show that compound 5 exhibits good brain exposure and potent 2-HG inhibition in a HT1080-derived mouse xenograft model, which makes it a potential preclinical candidate to treat IDH1-mutant brain tumors.
Access to enantiomerically enriched cis-2,3-disubstituted azetidines via diastereoselective hydrozirconation
Pradhan, Tarun K.,Krishnan, K. Syam,Vasse, Jean-Luc,Szymoniak, Jan
supporting information; experimental part, p. 1793 - 1795 (2011/06/19)
An asymmetric variant of the hydrozirconation reaction has been established starting from Boc-protected chiral allylic amines. The resulting diastereoselectively formed N-functionalized organozirconiums can be considered as promising chirons. In this case
A practical procedure for the multigram synthesis of the SuperQuat chiral auxiliaries
Bull, Steven D.,Davies, Stephen G.,Jones, Simon,Polywka, Mario E. C.,Shyam Prasad,Sanganee, Hitesh J.
, p. 519 - 521 (2007/10/03)
An efficient and simple synthesis of oxazolidin-2-one SuperQuat chiral auxiliaries is described which provides rapid access to multigram quantities of the auxiliaries.
