A Domino Reaction for the Synthesis of Novel 1,3-Dihydrofuro[3,4-c]pyridines from Pyridoxal and Ketones

A convenient domino route for the synthesis of novel 1,3-dihydrofuro[3,4-c]pyridines from pyridoxal and alkyl, aryl or heteroaryl ketones under basic conditions is reported. A series of nine derivatives is obtained in 53–90% yields after stirring reactants for 48 hours at room temperature. Most products are easily isolated by filtration followed by recrystallization from ethanol. All products were fully characterized by FTIR, HRMS, and 1H and 13C NMR spectroscopy. The X-ray crystal structure of a representative example of the 1,3-dihydrofuro[3,4-c]pyridine series is also presented.

Towards a RIOK2 Chemical Probe: Cellular Potency Improvement of a Selective 2-(Acylamino)pyridine Series

RIOK2 is an understudied kinase associated with a variety of human cancers including non-small cell lung cancer and glioblastoma. No potent, selective, and cell-active chemical probe currently exists for RIOK2. Such a reagent would expedite research into the biological functions of RIOK2 and validate it as a therapeutic target. Herein, we describe the synthesis of naphthyl-pyridine based compounds that have both improved cellular activity while maintaining selectivity for RIOK2.

Towards a RIOK2 Chemical Probe: Cellular Potency Improvement of a Selective 2-(Acylamino)pyridine Series

RIOK2 is an understudied kinase associated with a variety of human cancers including non-small cell lung cancer and glioblastoma. No potent, selective, and cell-active chemical probe currently exists for RIOK2. Such a reagent would expedite research into the biological functions of RIOK2 and validate it as a therapeutic target. Herein, we describe the synthesis of naphthyl-pyridine based compounds that have both improved cellular activity while maintaining selectivity for RIOK2.

Towards a RIOK2 chemical probe: cellular potency improvement of a selective 2-(acylamino)pyridine series

Modification of the 2-(acylamino)pyridine scaffold led to the identification of structure–activity relationships that improve RIOK2 cellular potency and maintain its selectivity.