97455-61-3Relevant articles and documents
Novel indirect AMP-activated protein kinase activators: Identification of a second-generation clinical candidate with improved physicochemical properties and reduced hERG inhibitory activity
Kuramoto, Kazuyuki,Sawada, Yuki,Yamada, Tomohiro,Nagashima, Takeyuki,Ohnuki, Kei,Shin, Takashi
, p. 452 - 465 (2020/09/09)
This study reports the synthesis and evaluation of novel indirect AMP-activated protein kinase (AMPK) activators. The series of compounds selectively inhibited cell growth in several human breast cancer cell lines by activating AMPK. We performed back-up medicinal chemistry synthetic research on ASP4132, a previously reported as a compound for clinical development that acts as an indirect AMPK activator. This led to the successful identification of 4-({4-[5-({1-[(5-ethoxypyrazin-2-yl)methyl]-4-fluoropiperidin-4-yl}methoxy)-3-methylpyridine-2-carbonyl]piperazin-1-yl}methyl)benzonitrile succinate (27b), a potent, highly aqueous soluble and metabolically stable compound in human hepatocytes. Compound 27b also showed weaker human Ether-a-go-go Related Gene (hERG) inhibitory activity than that of compound 13 and ASP4132. Therefore, 27b was a promising AMPK activator and a second-generation clinical candidate for treatment for human cancer.
6-n-Alkoxy-3-Pyridinecarboxaldehydes: New Intermediates to Liquid Crystals. Properties of Some Derivatives.
Barbera, J.,Melendez, E.,Romero, P.,Serrano, J. L.
, p. 259 - 268 (2007/10/02)
The synthesis of new intermediates to liquid crystals, a series of 6-n-alkoxy-3-pyridinecarboxaldehydes is described.The mesomorphic properties of their precursors, the 6-n-alkoxy-3-pyridinecarboxylic acids are reported.Some derivatives of the carboxaldeh