1219142-62-7Relevant academic research and scientific papers
VITAMIN RECEPTOR DRUG DELIVERY CONJUGATES FOR TREATING INFLAMMATION
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Page/Page column 94-95, (2011/07/09)
Described herein are compositions, methods, compounds, conjugates, and kits for use in targeted drug delivery using drug delivery conjugates containing hydrophilic spacer linkers for use in treating disease states caused by pathogenic cell populations, such as inflammatory cells.
Design and regioselective synthesis of a new generation of targeted therapeutics. Part 3: Folate conjugates of aminopterin hydrazide for the treatment of inflammation
Vlahov, Iontcho R.,You, Fei,Santhapuram, Hari Krishna R.,Wang, Yu,Vaughn, Jeremy F.,Hahn, Spencer J.,Kleindl, Paul J.,Fan, Mingjin,Leamon, Christopher P.
, p. 1202 - 1205 (2011/04/16)
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.
