Matsuoka H, Kato N, Ohi N, Miyamoto K, Mihara M, Takeda Y
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd., Shizuoka, Japan.
Chem Pharm Bull (Tokyo). 1997 Jul;45(7):1146-50. 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, Nb-(3-carboxyphenyl)-N alpha-[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.