Methotrexate analogs. 29. Effect of. gamma.-aminobutyric acid spacers between the pteroyl and glutamate moieties on enzyme binding and cell growth inhibition

…, RA Forsch, JH Freisheim, PV Danenberg…

文献索引：Rosowsky, Andre; Forsch, Ronald A.; Freisheim, James H.; Danenberg, Peter V.; Moran, Richard G.; Wick, Michael M. Journal of Medicinal Chemistry, 1986 , vol. 29, # 10 p. 1872 - 1876

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被引用次数: 6

摘要

A series of “stretched” methotrexate (MTX) analogues containing up to five 4-aminobutyryl (Gab) spacers between the 4-amino-4-deoxy-No-methylpteroyl (MeAPA) moiety and the glutamate (Glu) side chain was prepared. Interest in these compounds stemmed from their relationship to MTX y-polyglutamates, from which they differ only in lacking “internal” a- carboxyl groups. The ability of the MeAPA-Gab,-Glu derivatives to inhibit dihydrofolate ...