Methotrexate analog. 32. Chain extension,. alpha.-carboxyl deletion, and. gamma. carboxyl replacement by sulfonate and phosphate. Effect on enzyme binding and …

A Rosowsky, RA Forsch, RG Moran…

Index: Rosowsky; Forsch; Moran; Kohler; Freisheim Journal of Medicinal Chemistry, 1988 , vol. 31, # 7 p. 1326 - 1331

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Citation Number: 39

Abstract

Analogues of methotrexate (MTX) and aminopterin (AMT) with aminophosphonoalkanoic, aminoalkanesulfonic, and aminoalkanephosphonic acid side chains in place of glutamate were synthesized and tested as inhibitors of folylpolyglutamate synthetase (FPGS) from mouse liver. The aminophosphonoalkanoic acid analogues were also tested as inhibitors of dihydrofolate reductase (DHFR) from L1210 murine leukemia cells and as inhibitors of the ...