A step-wise synthetic approach is necessary to access γ-conjugates of folate: folate-conjugated prodigiosenes
| Autor: | Brandon R. Groves, Alison Thompson, Estelle Marchal, Carlotta Figliola |
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| Přispěvatelé: | Dalhousie University [Halifax] |
| Rok vydání: | 2019 |
| Předmět: |
Chemistry
[CHIM.ORGA]Chemical Sciences/Organic chemistry General Chemical Engineering 02 engineering and technology General Chemistry Glutathione Polyethylene glycol [CHIM.THER]Chemical Sciences/Medicinal Chemistry Conjugated system 010402 general chemistry 021001 nanoscience & nanotechnology 01 natural sciences Combinatorial chemistry 0104 chemical sciences 3. Good health chemistry.chemical_compound Folic acid Folate receptor Pharmacophore 0210 nano-technology ComputingMilieux_MISCELLANEOUS Conjugate |
| Zdroj: | RSC Advances RSC Advances, Royal Society of Chemistry, 2019, 9 (25), pp.14078-14092. ⟨10.1039/C9RA01435G⟩ |
| ISSN: | 2046-2069 |
| Popis: | Despite the vast literature that describes reacting folic acid with a pharmacophore, this route is ineffective in providing the correct regioisomer of the resulting conjugate. We herein present a step-wise route to the preparation of nine folate conjugates of the tripyrrolic prodigiosene skeleton. The strict requirement for step-wise construction of the folate core is demonstrated, so as to achieve conjugation at only the desired γ-carboxylic acid and thus maintain the α-carboxylic site for folate receptor (FRα) recognition. Linkages via ethylenediamine, polyethylene glycol and glutathione are demonstrated. |
| Databáze: | OpenAIRE |
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