| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1362193 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
Efficient syntheses of folate receptor (FR) targeting conjugates of the anti-inflammatory, aminopterin hydrazide, are described. 2-{4-Benzoylamino}-5-oxo-5-{N′-[2-(pyridin-2-yldisulfanyl)-ethoxycarbonyl]-hydrazino}-pentanoic acid is synthesized from commercially available 4-[(2-amino-4-imino-3,4-dihydro-pteridin-6-yl-methyl)-amino]-benzoic acid. Conjugation of this novel, activated aminopterin hydrazide to folic acid through cysteine-terminating (C-terminus), peptide/carbohydrate spacers results in highly water soluble conjugates which allow for the release of free aminopterin hydrazide within the endosomes of targeted cells.
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Related Topics
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Authors
Iontcho R. Vlahov, Fei You, Hari Krishna R. Santhapuram, Yu Wang, Jeremy F. Vaughn, Spencer J. Hahn, Paul J. Kleindl, Mingjin Fan, Christopher P. Leamon,