182344-63-4Relevant articles and documents
Synthesis of micrococcinic acid
Ross Kelly,Jagoe,Gu
, p. 4263 - 4266 (1991)
The first synthesis of micrococcinic acid (2) is described. The five rings of 2 are assembled from monocyclic precursors using four palladium-catalyzed biaryl coupling reactions.
Discovery of novel Bcr-Abl inhibitors with diacylated piperazine as the flexible linker
Pan, Xiaoyan,Dong, Jinyun,Shi, Yaling,Shao, Ruili,Wei, Fen,Wang, Jinfeng,Zhang, Jie
, p. 7050 - 7066 (2015/06/25)
Forty-two compounds (series 8, 9 and 10) incorporated with diacylated piperazine have been synthesized and evaluated as novel Bcr-Abl inhibitors based on 'six-atom linker'. Five of them, 8d, 8h, 8l, 10m and 10p, displayed potent Bcr-Abl inhibitory activity comparable with Imatinib. Moreover, compounds 8e, 10q, 10s, and 10u were potent Bcr-Abl inhibitors with IC50 values at the sub-micromolecular level. Most compounds exhibited moderate to high antiproliferative activity against K562 cells. In particular, compound 9e was the most promising Bcr-Abl inhibitor. Docking studies revealed that the binding modes of these compounds were similar with Imatinib. These compounds could be considered as promising lead compounds for further optimization.
Rapid and selective in situ reduction of pyridine- N -oxides with tetrahydroxydiboron
Londregan, Allyn T.,Piotrowski, David W.,Xiao, Jun
, p. 2695 - 2700 (2014/01/06)
Pyridine-N-oxides are often used as reactive precursors in the syntheses of substituted pyridines. Isolation and subsequent reduction of the associated pyridine-N-oxide intermediates can be challenging. We have discovered that tetrahydroxydiboron functions as a mild, versatile, and remarkably selective reducing agent for pyridine-N-oxides and may be used in an in situ fashion, thus obviating the isolation of N-oxide-containing intermediates. Georg Thieme Verlag Stuttgart New York.