Methotrexate analogs. 6. Replacement of glutamic acid by various amino acid esters and amines
- 1 September 1975
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 18 (9) , 909-912
- https://doi.org/10.1021/jm00243a010
Abstract
A series of methotrexate (MTX) analogs was prepared in which the glutamic acid moiety was replaced by various amino acid esters and amines. The synthetic method consisted of the reaction of 4-amino-4-deoxy-N10-methylpteroic acid with various reagents to form intermediate mixed anhydrides, which then reacted with amino acid esters or amines to give the MTX analogs. These compounds were tested for antibacterial activity against Streptococcus faecium and for antitumor activity against L1210 leukemia in mice. Several compounds showed significant antibacterial activity; the MTX homocysteinethiolactone and MTX aspartate analogs showed marginal in vivo antitumor activity.Keywords
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