43077-04-9Relevant academic research and scientific papers
SUBSTITUTED NUCLEOSIDE ANALOGUES FOR USE AS PRMT5 INHIBITORS
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Page/Page column 95; 96, (2017/09/27)
The present invention relates novel substituted nucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Hemisynthesis of deuteriated adenosylhopane and conversion into bacteriohopanetetrol by a cell-free system from Methylobacterium organophilum
Liu, Wenjun,Bodlenner, Anne,Rohmer, Michel
, p. 3393 - 3405 (2015/03/18)
Adenosylhopane is a putative precursor of the widespread bacterial C35 biohopanoids. A concise and flexible hemisynthesis of adenosylhopane has been developed including as key steps a cross metathesis between two olefins containing either the h
Analogues of the natural product sinefungin as inhibitors of EHMT1 and EHMT2
Devkota, Kanchan,Lohse, Brian,Liu, Qing,Wang, Ming-Wei,Staerk, Dan,Berthelsen, Jens,Clausen, Rasmus Praetorius
supporting information, p. 293 - 297 (2014/05/06)
A series of analogues of the natural product sinefungin lacking the amino acid moiety was synthesized and probed for their ability to inhibit EHMT1 and EHMT2. This study led to inhibitors 3b and 4d of methyltransferase activity of EHMT1 and EHMT2 and it demonstrates that such analogues constitute an interesting scaffold to develop selective methyltransferase inhibitors. Surprisingly, the inhibition was not competitive toward AdoMet.
Stereoselective adenylate deaminase (5′-adenylic acid deaminase, AMPDA)-catalyzed deamination of 5′-alkyl substituted adenosines: A comparison with the action of adenosine deaminase (ADA)
Ciuffreda, Pierangela,Loseto, Angela,Santaniello, Enzo
, p. 203 - 206 (2007/10/03)
The enzymes adenylate deaminase (AMPDA) and adenosine deaminase (ADA) are able to catalyze the stereoselective hydrolytic deamination of (5′R,S)-methyl-2′,3′-isopropylidene adenosine, but the 5′-butyl analog is a substrate only for AMPDA, which stereospec
