85803-27-6

Upstream product

• 85803-25-4 di-tert-butyl N-(2-fluoro-4-nitrobenzoyl)-l-glutamate 
• 446-31-1 2-fluoro-4-aminobenzoic acid 
• 32677-01-3 L-glutamic acid di-tert-butyl ester hydrochloride 
• 1427-07-2 2-fluoro-4-nitrotoluene 
• 403-23-6 2-fluoro-4-nitrobenzoyl chloride 
• 403-24-7 2-fluoro-4-nitrobenzoic acid 

Downstream Products

• 129175-67-3 di-tert-butyl N-<2-fluoro-4-<(2-phthalimidoethyl)amino>benzoyl>-L-glutamate 
• 85803-30-1 2'-fluoroaminopterin di-tert-butyl ester 
• 129175-68-4 (S)-2-[4-(Cyanomethyl-amino)-2-fluoro-benzoylamino]-pentanedioic acid di-tert-butyl ester 
• 157665-26-4 di-tert-butyl <2-fluoro-4-benzoyl>-L-glutamate 
• 85803-29-8 2'-fluoroaminopterin 
• 129175-60-6 (S)-2-{4-[[2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-ethyl]-(2-methyl-4-oxo-3,4-dihydro-quinazolin-6-ylmethyl)-amino]-2-fluoro-benzoylamino}-pentanedioic acid di-tert-butyl ester 
• 129175-21-9 N-(4-{N-[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]-N-(2-aminoethyl)amino}-2-fluorobenzoyl)-L-glutamic acid 
• 129175-61-7 (S)-2-{4-[Cyanomethyl-(2-methyl-4-oxo-3,4-dihydro-quinazolin-6-ylmethyl)-amino]-2-fluoro-benzoylamino}-pentanedioic acid di-tert-butyl ester 
• 129175-22-0 N-(4-{N-[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]-N-(cyanomethyl)amino}-2-fluorobenzoyl)-L-glutamic acid 
• 126632-26-6 N-<4-<<3-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)propyl>amino>-2-fluorobenzoyl>-L-glutamic acid 
• 157665-27-5 di-tert-butyl <2-fluoro-4-amino>benzoyl>-L-glutamate 
• 157665-28-6 di-tert-butyl <2-fluoro-4-<(2-chloroethyl)<2-(mesyloxy)ethyl>amino>benzoyl>-L-glutamate 
• 157665-29-7 di-tert-butyl <2-fluoro-4-benzoyl>-L-glutamate 

Relevant academic research and scientific papers

Synthesis and structure-activity relationships of TAN-1511 analogues as potent hematopoietic agents

A series of TAN-1511 analogues bearing a non-peptide spacer in place of the Gly-Gly-Gly sequence in the peptide moiety was synthesized, and the effects of these compounds on the proliferation of bone marrow cells in culture and experimental leukocytopenia in mice were examined. The structure- activity relationships obtained were as follows. As the substituent at the 2- position of the 4-thiabeptanoic acid framework, an amino group, methyl group or hydrogen was preferable; as a spacer in place of the Gly-Gly-Gly sequence, a 4-aminobenzoyl or 4-aminomethylbenzoyl group was suitable; and as the fatty acids bonded to the 6,7-dihydroxy groups, C16 fatty acid was best. Compounds 12f, 30d and 30i potently promoted the proliferation of bone marrow cells in culture and the restoration of leukocyte counts in a murine leukocytopenia model.

Novel prodrugs of alkylating agents derived from 2-fluoro- and 3- fluorobenzoic acids for antibody-directed enzyme prodrug therapy

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

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.