27512-72-7Relevant academic research and scientific papers
Discovery of substituted indole derivatives as allosteric inhibitors of m6A-RNA methyltransferase, METTL3-14 complex
Jin, Mi Sun,Kim, Subin,Kim, Yong-Chul,Lee, Je-Heon
, (2022/01/20)
m6A RNA methyltransferase (METTL3-14) catalyzes the methylation of adenosine in mRNA and plays important roles in mRNA functions, and it has been implicated in the progression of multiple cancers, including acute myeloid leukemia (AML). In this study, we describe the discovery of the first allosteric inhibitor of the METTL3-14 complex based on structure–activity relationship (SAR) and optimization studies of the hit compound, 4-[2-[5-chloro-1-(diphenylmethyl)-2-methyl-1H-indol-3-yl]-ethoxy]benzoic acid (CDIBA). Compound 43n was optimized throughout the modifications of 4 different regions of the structure, and it displayed potent enzyme inhibitory activity of the METTL3-14 complex (IC50?=?2.81 μM) and an antiproliferative effect in the AML cell lines by suppressing the m6A level of mRNA. The inhibition mechanism and binding mode of 43n were based on the interaction of the reversible and noncompetitive inhibitory profile at the allosteric site along with selectivity for the METTL3-14 complex relative to each subunit enzyme or truncated complex enzyme.
Patch preparations for treating plants
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, (2008/06/13)
The following invention introduces a patch preparation for treating plants, whereas the patch preparations comprise a chemical layer composed of at least one agrochemically active compound, at least one adhesive and optionally, one or more additives. The components are dispersed in a matrix state on a substrate which are then introduced on the roots of the plant to be treated.
Orally Active Aldose Reductase Inhibitors: Indazoleacetic, Oxopyridazineacetic, and Oxopyridopyridazineacetic Acid Derivatives
Mylari, Banavara L.,Zembrowski, William J.,Beyer, Thomas A.,Aldinger, Charles E.,Siegel, Todd W.
, p. 2155 - 2162 (2007/10/02)
Benzothiazole side chains featured in zopolrestat (1a) and its congeners were incorporated into oxophthalazineacetic acid replacements, including indazole, pyridazinone, and pyridopyridazinone with a pendant acetic acid moiety.Potent aldose reductase inhi
Method for thinning young fruits and blossoms and agent therefor
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, (2008/06/13)
Method for thinning young fruits and blossoms by applying to fruit trees, particularly citrus fruit trees an indazole compound of the formula: STR1 wherein R is hydrogen or a lower alkyl having 1 to 4 carbon atoms, and X is a halogen, or the salt thereof, and a thinning agent containing as the active ingredient the indazole compound as mentioned above.
