Antirheumatic agents. III. Novel methotrexate derivatives bearing an indoline ring and a modified ornithine or glutamie acid

DOI: 10.1248/cpb.45.1146

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1146 - 1150 (1997)

Update date:2022-07-29

Topics:

Authors:

Matsuoka, Hiroharu

Kato, Nobuaki

Ohi, Nobuhiro

Miyamoto, Katsuhito

Mihara, Masahiko

Takeda, Yasuhisa

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Article abstract of DOI:10.1248/cpb.45.1146

The synthesis, biological profile and structure-activity relationship of various methotrexate (MTX) derivatives bearing an indoline ring are described. In particular, Nδ-(3-carboxyphenyl)-Nα-[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.

Full text of DOI:10.1248/cpb.45.1146

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