194809-05-7Relevant academic research and scientific papers
BENZAZOLE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE AS AURORA KINASE INHIBITORS
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Page/Page column 66-67, (2010/11/28)
The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.
Synthesis and evaluation of novel fluorinated methotrexate derivatives for application to rheumatoid arthritis treatment
Kokuryo, Yoshitsugu,Kawata, Kyozo,Nakatani, Takuji,Kugimiya, Akira,Tamura, Yoshinori,Kawada, Kenji,Matsumoto, Mitsunobu,Suzuki, Ryuji,Kuwabara, Kenji,Hori, Yozo,Ohtani, Mitsuaki
, p. 3280 - 3291 (2007/10/03)
In ongoing search for new antifolate drugs useful against rheumatoid arthritis (RA) led us to prepare new methotrexate (MTX) derivatives containing enantiomerically pure L-erythro- or L-threo-γ-fluoroglutamic acid. The derivatives in which the phenyl ring was replaced by a 3'- substituted phenyl or methylthiophene ring showed potent immunosuppressive activities, including in vitro inhibition of mitogen responses of both T and B cells and in vivo inhibition of antibody production in mice. These compounds also exhibited inhibitory activity in adjuvant arthritis in rats. Their toxicity was lower than that of MTX, which was probably due to the strong electronegativity of fluorine, which increases the acidity of the γ- carboxyl group and thereby decreases polyglutamylation in normal cells. These results revealed the potential of the fluorinated MTX derivatives as candidate drugs for the treatment of RA.
