260050-97-3Relevant academic research and scientific papers
HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME
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Paragraph 00148, (2015/01/16)
Disclosed are compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein Y, Ra, Ra', Rc, Rf, X2, Rd, Rd', Re, Re', m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular and neurodegenerative diseases or disorders.
Fragment screening and assembly: A highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor
Liu, Gang,Xin, Zhili,Pei, Zhonghua,Hajduk, Philip J.,Abad-Zapatero, Cele,Hutchins, Charles W.,Zhao, Hongyu,Lubben, Thomas H.,Ballaron, Stephen J.,Haasch, Deanna L.,Kaszubska, Wiweka,Rondinone, Cristina M.,Trevillyan, James M.,Jirousek, Michael R.
, p. 4232 - 4235 (2007/10/03)
Using an NMR-based fragment screening and X-ray crystal structure-based assembly, starting with millimolar ligands for both the catalytic site and the second phosphotyrosine binding site, we have identified a small-molecule inhibitor of protein tyrosine phosphatase 1B with low micromolar inhibition constant, high selectivity (30-fold) over the highly homologous T-cell protein tyrosine phosphatase, and good cellular activity in COS-7 cells.
Alkynyl-substituted quinolin-2-one derivatives useful as anticancer agents
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, (2008/06/13)
The present invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are as defined herein. The above compounds of formula 1 are useful in
