Brasca, Maria Gabriella published the artcilePyrrole-3-carboxamides as potent and selective JAK2 inhibitors, Safety of (5-Chloro-2-(trifluoromethyl)phenyl)boronic acid, the publication is Bioorganic & Medicinal Chemistry (2014), 22(17), 4998-5012, database is CAplus and MEDLINE.
We report herein the discovery, structure guided design, synthesis and biol. evaluation of a novel class of JAK2 inhibitors. Optimization of the series led to the identification of the potent and orally bioavailable JAK2 inhibitor (I; NMS-P953). I displayed significant tumor growth inhibition in SET-2 xenograft tumor model, with a mechanism of action confirmed in vivo by typical modulation of known biomarkers, and with a favorable pharmacokinetic and safety profile.
Bioorganic & Medicinal Chemistry published new progress about 1195945-67-5. 1195945-67-5 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic Acids,Boronic acid and ester, name is (5-Chloro-2-(trifluoromethyl)phenyl)boronic acid, and the molecular formula is C7H5BClF3O2, Safety of (5-Chloro-2-(trifluoromethyl)phenyl)boronic acid.
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