61655-77-4Relevant articles and documents
Novel Pim Kinase Inhibitor and Uses Thereof
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Paragraph 0117; 0141-0150; 0173-0178, (2021/09/14)
The present invention relates to novel Pim kinase inhibitors and uses thereof. A novel Pim oxydol 1, 3, 4 - (3H) -2 thione (1, 4-2 (3H) Oxadiazole) - based compound having - thione kinase inhibitory activity and a composition for inhibiting Pim kinase or a composition for preventing or treating cancer comprising the same are provided. Since the 1, 3, 4 - oxydol -2 (3H) - thione (1, 4-Oxadiazole-2 (3H) - thione) - based compound of the present invention has a very effective Pim kinase inhibitory activity even at low concentrations, the compound of the present invention can be useful as a composition for preventing or treating cancer through Pim kinase inhibition.
Selective mono-amination of dichlorodiazines
Sengmany, Stéphane,Lebre, Julie,Le Gall, Ewan,Léonel, Eric
, p. 4859 - 4867 (2015/08/03)
A mild, easy-to-perform, and versatile method for the formation of aminochlorodiazines from reaction of several types of dichlorodiazines (i.e., pyridazines, pyrimidines, and pyrazines) with primary or secondary amines in ethanol in the presence of trieth
Hit to lead account of the discovery of a new class of inhibitors of pim kinases and crystallographic studies revealing an unusual kinase binding mode
Qian, Kevin,Lian, Wang,Cywin, Charles L.,Farmer, Bennett T.,Hickey, Eugene,Homon, Carol,Jakes, Scottm,Kashem, Mohammed A.,Lee, George,Leonard, Scott,Jun, Li,Magboo, Ronald,Wang, Mao,Pack, Edward,Peng, Charlene,Prokopowicz, Anthony,Welzel, Morgan,Wolak, John,Morwick, Tina
experimental part, p. 1814 - 1827 (2009/12/31)
A series of inhibitors of Pim-2 kinase identified by high-throughput screening is described. Details of the hit validation and lead generation process and structure-activity relationship (SAR) studies are presented. Disclosure of an unconventional binding mode for 1, as revealed by X-ray crystallography using the highly homologous Pim-1 protein, is also presented, and observed binding features are shown to correlate with the Pim-2 SAR. While highly selective within the kinase family, the series shows similar potency for both Pim-1 and Pim-2, which was expected on the basis of homology, but unusual in light of reports in the literature documenting a bias for Pim-1. A rationale for these observations based on Pim-1 and Pim-2 KM(ATP) values is suggested. Some interesting cross reactivity with casein kinase-2 was also identified, and structural features which may contribute to the association are discussed.