cb-3705 and 5-8-dideazaisofolic-acid

cb-3705 has been researched along with 5-8-dideazaisofolic-acid* in 1 studies

Other Studies

1 other study(ies) available for cb-3705 and 5-8-dideazaisofolic-acid

ArticleYear
In vitro metabolism of 5,8-dideazafolates and 5,8-dideazaisofolates by mammalian folylpoly-gamma-glutamate synthetase.
    Biochemical pharmacology, 1991, Jul-25, Volume: 42, Issue:4

    The in vitro metabolism of a variety of 5,8-dideazafolate and 5,8-dideazaisofolate analogues by pig liver folylpolyglutamate synthetase and the specificity of the enzyme for some polyglutamate derivatives of these analogues have been investigated. All 4-oxo-quinazoline analogues were metabolized to long chain polyglutamate derivatives, primarily the pentaglutamate, whereas 4-amino-quinazolines were metabolized to a lesser extent, with the accumulation of di- and triglutamate derivatives. This pattern of metabolism was consistent with the large drop in Vmax/Km and Vmax values for folylpolyglutamate synthetase observed with diglutamate derivatives of 4-aminofolate analogues. The extent of metabolism of the various analogues did not correlate with the relative substrate effectiveness of their parent monoglutamate derivatives. The 5-chloro and 5-methyl substitutions of quinazolines enhanced the addition of glutamate residues to 4-amino derivatives but markedly impaired the metabolism of 4-oxo derivatives.

    Topics: Aminopterin; Animals; Folic Acid Antagonists; Kinetics; Liver; Peptide Synthases; Pteroylpolyglutamic Acids; Quinazolines; Structure-Activity Relationship; Substrate Specificity

1991