27058-48-6Relevant articles and documents
Discovery of wtRET and V804MRET Inhibitors: From Hit to Lead
Mologni, Luca,Dalla Via, Martina,Chilin, Adriana,Palumbo, Manlio,Marzaro, Giovanni
supporting information, p. 1390 - 1398 (2017/09/01)
Oncogenic activation of RET kinase has been found in several neoplastic diseases, like medullary thyroid carcinoma, multiple endocrine neoplasia, papillary thyroid carcinoma, and non-small-cell lung cancer. Currently approved RET inhibitors were not originally designed to be RET inhibitors, and their potency against RET kinase has not been optimized. Hence, novel compounds able to inhibit both wild-type RET (wtRET) and its mutants (e.g., V804MRET) are needed. Herein we present the development and the preliminary evaluation of a new sub-micromolar wtRET/V804MRET inhibitor, N-(2-fluoro-5-trifluoromethylphenyl)-N′-{4′-[(2′′-benzamido)pyridin-4′′-ylamino]phenyl}urea (69), endowed with a 4-anilinopyridine structure, starting from our previously identified 4-anilinopyrimidine hit compound. Profiling against a panel of kinases indicated 69 as a multi cKIT/wtRET/V804MRET inhibitor.
PYRIMIDINES USEFUL AS MODULATORS OF VOLTAGE-GATED ION CHANNELS
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Page 129-130, (2010/02/10)
The present invention relates to compounds useful as inhibitors of voltage-gated ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Regioselective Synthesis of Pyrimidines from Ketene Dithioacetals or Alkoxymethylene Compounds
Lorente, Antonio,Vaquerizo, Laura,Martin, Avelino,Gomez-Sal, Pilar
, p. 71 - 86 (2007/10/02)
Regioselective cyclizations of the condensation products obtained by the reaction of nitrogen nucleophiles with ketene dithioacetals or alkoxymethylene compounds are reported.Stereoelectronic factors or geometry of the carbon-carbon double bond determine