50794-16-6Relevant academic research and scientific papers
Identification and characterization of the first fragment hits for SETDB1 Tudor domain
Mader,Mendoza-Sanchez, Rodrigo,Iqbal, Aman,Dong, Aiping,Dobrovetsky,Corless, Victoria B.,Liew, Sean K.,Houliston, Scott R.,De Freitas, Renato Ferreira,Smil,Sena, Carlo C. Dela,Kennedy, Steven,Diaz, Diego B.,Wu, Hong,Dombrovski, Ludmila,Allali-Hassani, Abdellah,Min, Jinrong,Schapira, Matthieu,Vedadi, Masoud,Brown, Peter J.,Santhakumar, Vijayaratnam,Yudin, Andrei K.,Arrowsmith, Cheryl H.
, p. 3866 - 3878 (2019/07/23)
SET domain bifurcated protein 1 (SETDB1) is a human histone-lysine methyltransferase which is amplified in human cancers and was shown to be crucial in the growth of non-small and small cell lung carcinoma. In addition to its catalytic domain, SETDB1 harb
Towards Gram-negative antivirulence drugs: New inhibitors of HldE kinase
Desroy, Nicolas,Moreau, Francois,Briet, Sophia,Fralliec, Geraldine Le,Floquet, Stephanie,Durant, Lionel,Vongsouthi, Vanida,Gerusz, Vincent,Denis, Alexis,Escaich, Sonia
experimental part, p. 1276 - 1289 (2009/07/11)
Gram-negative bacteria lacking heptoses in their lipopolysaccharide (LPS) display attenuated virulence and increased sensitivity to human serum and to some antibiotics. Thus inhibition of bacterial heptose synthesis represents an attractive target for the development of new antibacterial agents. HldE is a bifunctional enzyme involved in the synthesis of bacterial heptoses. Development of a biochemical assay suitable for high-throughput screening allowed the discovery of inhibitors 1 and 2 of HldE kinase. Study of the structure-activity relationship of this series of inhibitors led to highly potent compounds.
Optionally substituted 1,2,3,5-tetrahydroimidezo(2,1-b)-quinazolin-2-ones and 6(H)-1,2,3,4-tetrahydropyimido(2,1-b)quinazolin-2-ones
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, (2008/06/13)
Optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]-quinazolin-2-ones and 6-[H]-1,2,3,4-tetrahydropyrimido[2,1-b]-quinazolin-2-ones or the pharmaceutically acceptable salts thereof are compounds useful as blood platelet anti-aggregative and/or antihypertensive and/or bronchodilator agents in mammals, including humans.
Process for the preparation of optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones
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, (2008/06/13)
A new process has been developed for the synthesis of optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones.
