39774-28-2Relevant articles and documents
Conversion from arenes having a benzene ring to those having a picolinic acid by simple growing cell reactions using Escherichia coli that expressed the six bacterial genes involved in biphenyl catabolism
Shindo, Kazutoshi,Osawa, Ayako,Nakamura, Ryoko,Kagiyama, Yukiko,Sakuda, Shohei,Shizuri, Yoshikazu,Furukawa, Kensuke,Misawa, Norihiko
, p. 15042 - 15043 (2004)
The comprehensive bioconversion of aromatic compounds with a benzene ring to a picolinic acid was achieved with a recombinant Escherichia coli strain that expressed the six genes involved in biphenyl catabolism, these being the bphA1(2072)A2A3A4 genes encoding the evolved biphenyl dioxygenase, the bphB gene encoding dihydrodiol dehydrogenase, and the bphC gene encoding catechol 2,3-dioxygenase. Copyright
Discovery of pyrrolopyridine-pyridone based inhibitors of met kinase: Synthesis, X-ray crystallographic analysis, and biological activities
Kyoung, Soon Kim,Zhang, Liping,Schmidt, Robert,Cai, Zhen-Wei,Wei, Donna,Williams, David K.,Lombardo, Louis J.,Trainor, George L.,Xie, Dianlin,Zhang, Yaquan,An, Yongmi,Sack, John S.,Tokarski, John S.,Darienzo, Celia,Kamath, Amrita,Marathe, Punit,Zhang, Yueping,Lippy, Jonathan,Jeyaseelan Sr., Robert,Wautlet, Barri,Henley, Benjamin,Gullo-Brown, Johnni,Manne, Veeraswamy,Hunt, John T.,Fargnoli, Joseph,Borzilleri, Robert M.
experimental part, p. 5330 - 5341 (2009/07/01)
Conformationally constrained 2-pyridone analogue 2 is a potent Met kinase inhibitor with an IC50 value of 1.8 nM. Further SAR of the 2-pyridone based inhibitors of Met kinase led to potent 4-pyridone and pyridine N-oxide inhibitors such as 3 and 4. The X-ray crystallographic data of the inhibitor 2 bound to the ATP binding site of Met kinase protein provided insight into the binding modes of these inhibitors, and the SAR of this series of analogues was rationalized. Many of these analogues showed potent antiproliferative activities against the Met dependent GTL-16 gastric carcinoma cell line. Compound 2 also inhibited Flt-3 and VEGFR-2 kinases with IC50 values of 4 and 27 nM, respectively. It possesses a favorable pharmacokinetic profile in mice and demonstrates significant in vivo antitumor activity in the GTL-16 human gastric carcinoma xenograft model.
A long-range chiral relay via tertiary amide group in asymmetric catalysis: new amino acid-derived N,P-ligands for copper-catalysed conjugate addition.
Malkov, Andrei V,Hand, John B,Kocovsky, Pavel
, p. 1948 - 1949 (2007/10/03)
New N,P-ligands 4-6, derived from valinol and prolinol, respectively, have been developed for the asymmetric, copper(I)-catalysed conjugate addition of diethylzinc to unsaturated ketones; the tertiary amide group has been shown to effectively relay the chiral information from the ligand backbone to the active centre.
