85803-25-4Relevant academic research and scientific papers
Novel prodrugs of alkylating agents derived from 2-fluoro- and 3- fluorobenzoic acids for antibody-directed enzyme prodrug therapy
Springer,Niculescu-Duvaz,Pedley
, p. 2361 - 2370 (2007/10/02)
The synthesis of six novel fluorinated potential prodrugs for antibody- directed enzyme prodrug therapy is described. The [2- and 3-fluoro-4-[bis(2- chloroethyl)amino]benzoyl]-L-glutamic acid (9 and 21), their bis(mesyloxy)ethyl derivatives (7 and 19), an
Novel Fluorinated Antifolates. Enzyme Inhibition and Cytotoxicity Studies on 2'- and 3'-Fluoroaminopterin
Henkin, Jack,Washtien, Wendy L.
, p. 1193 - 1196 (2007/10/02)
Two novel analogues of aminopterin with a single fluorine substitution in the 2' (compound 8) or in the 3' (compound 9) position of the p-aminobenzoyl group were synthesized and evaluated as inhibitors of dihydrofolate reductase from two bacterial species and from human HeLa cells.The 2'fluoro compound was bound essentially the same as aminopterin itself, while the 3'-fluoro derivative bound two- to threefold more tightly in all cases.UV spectral shifts indicated normal binding of the pteridine.Cytotoxicity studies against mouse leukemia L1210 cells and the human stomach cancer line HuTu80 indicated equivalent toxicity of the parent drug with the 2'-fluoro analogue. 3'-Fluoroaminopterin was, however, twice as toxic as aminopterin to both cell lines.
