Discovery of 1-((6-Aminopyridin-3-yl)Methyl)-3-(4-Bromophenyl)Urea as a Potent, Irreversible Myeloperoxidase Inhibitor
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منابع مشابه
Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.
The mTOR mediated PI3K/AKT/mTOR signal transduction pathway has been demonstrated to play a key role in a broad spectrum of cancers. Starting from the mTOR selective inhibitor 1 (Torin1), a focused medicinal chemistry effort led to the discovery of an improved mTOR inhibitor 3 (Torin2), which possesses an EC(50) of 0.25 nM for inhibiting cellular mTOR activity. Compound 3 exhibited 800-fold sel...
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Abstract- Some new 3-(alkylsulfanyl)- 7-chloro-1-phenyl-1H-pyridazino [4,3-e][1,3,4]thiadiazine were synthesized by treatment of the alkyl-2-phenylhydrazinecarbodithioates with 4-bromo-3,6-dichloropyridazine in alkaline acetonitril. Orientation of the reaction has been determined by X-Ray crystallography technique. The chlorine atom on the number 7 position of these products was repla...
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Some new 3-(alkylsulfanyl)- 7-chloro-1-phenyl-1H-pyridazino [4,3-e][1,3,4]thiadiazine were synthesized by treatment of the alkyl-2-phenylhydrazinecarbodithioates with 4-bromo-3,6-dichloropyridazine in alkaline acetonitril. Orientation of the reaction has been determined by X-Ray crystallography technique. The chlorine atom on the number 7 position of these products was replaced by secondary am...
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The indoles plant growth hormones have exhibited potentially antitumor activities. However, the targets of these indoles have not been clearly elucidated. By introduction of hydroxamic acid group to the structure of indolebutyric acid, the derived molecule (IBHA) exhibited potent HDAC2 (IC50 value of 0.32 ± 0.02 µM) and HDAC3 (IC50 value of 0.14 ± 0.01 µM) inhibitory activities compared with SA...
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ژورنال
عنوان ژورنال: Journal of Pharmacology and Experimental Therapeutics
سال: 2018
ISSN: 0022-3565,1521-0103
DOI: 10.1124/jpet.118.248435