Antirheumatic Agents. III. Novel Methotrexate Derivatives Bearing an Indoline Ring and a Modified Ornithine or Glutamic Acid

Hiroharu MATSUOKA; Nobuaki KATO; Nobuhiro OHI; Katsuhito MIYAMOTO; Masahiko MIHARA; Yasuhisa TAKEDA

doi:10.1248/cpb.45.1146

Hiroharu MATSUOKA, Nobuaki KATO, Nobuhiro OHI, Katsuhito MIYAMOTO, Masahiko MIHARA, Yasuhisa TAKEDA

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Keywords: methotrexate, MX-9, indoline, anti-proliferation

JOURNAL FREE ACCESS

1997 Volume 45 Issue 7 Pages 1146-1150

DOI https://doi.org/10.1248/cpb.45.1146

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Abstract

The synthesis, biological profile and structure-activity relationship of various methotrexate (MTX) derivatives bearing an indoline ring are described. In particlular, N^δ-(3-carboxyphenyl)-N^α-[1-[(2, 4-diaminopteridin-6-yl)-methyl]indoline-5-ylcarbonyl]-L-glutamine (3d), compared to MTX, exhibited an enhanced anti-proliferative effect on human peripheral blood mononuclear cells obtained from healthy volunteers.

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