BTB-1 A small molecule inhibitor of the mitotic motor protein kif18A
Turning the motor off: A malachite green based assay leads to the identification of BTB-1 (see picture), the first small-molecule inhibitor of the mitotic motor protein Kif18A. BTB-1 reversibly inhibits the ATPase activity of the recombinant motor domain
Catarinella, Mario,Gruener, Tamara,Strittmatter, Tobias,Marx, Andreas,Mayer, Thomas U.
supporting information; experimental part
p. 9072 - 9076
(2010/03/03)
Proximity Effects in Diaryl Derivatives. Part 7. Mechanism of Base-catalysed Rearrangement of 2-(Hydroxyamino)aryl Phenyl Sulphones to 2-Hydroxy-2'-(phenylsulphonyl)azoxybenzenes
Base-catalysed rearrangement of a 2-(hydroxyamino)aryl phenyl sulphone (1b) to the 2-hydroxy-2'-(phenylsulphonyl)azoxybenzene (4b) was shown by isolation and kinetic studies to be a rapid reaction requiring oxygen; in the absence of oxygen the sulphur-free azoxybenzene (3; R=Cl) was the only product isolated from the reaction of (1c).A mechanism for the formation of 2-hydroxyazoxybenzenes (4) is proposed (Scheme 2) involving dimerization of a nitrosoaryl radical anion (9) to the dianion of an NN-diol (10), and displacement of a phenylsulphonyl group by intramolecular transfer of oxygen from a nitrogen atom.A similar study of the base-catalysed reactions of a 2-(hydroxyamino)aryl phenyl sulphide (12) in the presence of oxygen showed that with a poorer leaving group the bis(phenylthio)azoxybenzene (11; R=SPh) is formed.An improved procedure for the preparation of N-arylhydroxylamines from nitrobenzenes is described.
Cummings, Robert J.,Grundon, Michael F.,Knipe, Anthony C.,Wasfi, Adil S.
p. 105 - 108
(2007/10/02)
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