61655-77-4Relevant academic research and scientific papers
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.
1,3,4-Oxadiazole-2(3H)-thione Analogs as PIM Kinase Inhibitors
Choo, Hyeonseong,Hong, Victor Sukbong,Jeong, Seungik,Lee, Jinho,Won, Jongin,Yun, Yanghwan
, p. 994 - 1001 (2020/10/02)
Proviral integration site for moloney murine leukemia virus (PIM) kinases are highly expressed in hematological cancers. They phosphorylate downstream substrates that contribute to tumor growth and survival. Therefore, a potent inhibitor of PIM kinases is expected to be effective at treating hematological cancers. In the present study, several indole derivatives of 1,3,4-oxadiazole-2(3H)-thione were synthesized and evaluated as PIM kinase inhibitors. Structure–activity relationship studies yielded potent inhibitors of all three PIM kinases in the single-digit to low double-digit nanomolar IC50 range. Kinase profiling of a representative compound showed high selectivity among 15 other kinases.
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
Synthesis and evaluation of 5-(3-(Pyrazin-2-yl)benzylidene)thiazolidine-2,4-dione derivatives as pan-pim kinases inhibitors
Lee, Jinho,Park, Jongseong,Hong, Victor Sukbong
, p. 906 - 914 (2014/12/11)
Pim kinases play a key role in the regulation of signaling pathways including proliferation, migration, and metabolism and are a potential target for cancer therapy. A series of 5-benzylidenethiazolidine-2,4-diones were synthesized as pim kinase inhibitor
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.
AROMATIC AMIDES AS INHIBITORS OF C-FMS KINASE
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Page/Page column 76, (2008/06/13)
The invention relates to compounds of Formula (I), wherein A, X, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula (I), are also provided.
Piperazinylpyrazines
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, (2008/06/13)
Substituted piperazinylpyrazines and pharmaceutically acceptable salts thereof which have pharmacological activity as anorexigenic agents.
