… . 31. Meta and ortho isomers of aminopterin, compounds with a double bond in the side chain, and a novel analog modified at the. alpha.-carbon: chemical and in vitro …

A Rosowsky, H Bader, RA Forsch…

Index: Rosowsky, Andre; Bader, Henry; Forsch, Ronald A.; Moran, Richard G.; Freisheim, James H. Journal of Medicinal Chemistry, 1988 , vol. 31, # 4 p. 763 - 768

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Citation Number: 10

Abstract

Five heretofore undescribed analogues of methotrexate (MTX) and aminopterin (AMT) were synthesized and tested as dihydrofolate reductase (DHFR) inhibitors and tumor cell growth inhibitors. The meta isomer of AMT was obtained from 2, 4-diamino-B (bromomethyl) pteridine and m-(aminobenzoy1)-bglutamic acid, while the ortho isomer was obtained via the same route by using a-methyl y-tert-butyl o-(aminobenzoy1)-L-glutamate instead of the ...