107496-46-8Relevant articles and documents
Synthesis of [Hexafluorovalyl1,1′]gramicidin S
Arai, Toru,Imachi, Takashi,Kato, Tamaki,Ogawa, H. Iyehara,Fujimoto, Tsutomu,Nishino, Norikazu
, p. 1383 - 1389 (1996)
[Hexafluorovalyl1,1′]gramicidin S (8), in which two valine residues in the natural gramicidin S were replaced by L-hexafluorovaline (Hfv) residues, was synthesized by the solid-phase-synthesis and cyclization-cleavage method on benzophenone oxime resin. Though the racemic hexafluorovaline derivative was employed for the peptide synthesis, the desired product was isolated in moderate yield, probably reflecting the stable cyclic structure of 8. CD and 1HNMR spectra indicated that the conformation of 8 is similar to that of gramicidin S. The two β-turn structure and antiparallel β-sheet structure with four intramolecular hydrogen bondings were maintained in spite of introducing the hexafluorovaline residues. The dye-release experiment from lecithin vesicle and antimacrobial activity assay also indicated that 8 showed membrane-disturbing activity like gramicidin S, although the activity of 8 was somewhat weaker than gramicidin S.
METHOD FOR INHIBITING PROLIFERATION OF TUMOR CELLS
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Page/Page column 30, (2008/12/08)
Disclosed are methods for synergistically inhibiting the proliferation of tumor cells by contacting the tumor cells with a MEK inhibitor compound and erlotinib, either sequentially or simultaneously. Also disclosed are methods for inhibiting the proliferation of tumor cells in a human, by administering to the human, sequentially or simultaneously, an amount of erlotinib and a MEK inhibitor compound, wherein the amounts are effective, in combination, to synergistically inhibit the proliferation of the tumor cells in the human.
Substituted hydantoins
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Page/Page column 32, (2008/06/13)
The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.