56059-28-0Relevant academic research and scientific papers
Stealth recombinant human serum albumin nanoparticles conjugating 5-fluorouracil augmented drug delivery and cytotoxicity in human colon cancer, HT-29 cells
Sharma, Ankita,Kaur, Amanpreet,Jain, Upendra Kumar,Chandra, Ramesh,Madan, Jitender
, p. 200 - 208 (2017)
Background and objective 5-Fluorouracil (5-FU) is a first-line chemotherapeutic drug in colorectal cancer. However, intravenous administration of 5-FU at the dose of 7–12?mg/kg exhibits curbs like short half-life (20?min) and toxic side-effects on bone marrow cells. Therefore, in present investigation, 5-FU was conjugated to poly (ethylene glycol) anchored recombinant human serum albumin nanoparticles (5-FU-rHSA-PEG-NPs) to improve the pharmacokinetic and therapeutic profiles. Methods and results The mean particle size of 5-FU-rHSA-NPs was measured to be 44.3?±?5.8-nm, significantly (P??0.05) up to 48?h. However, addition of 20% v/v serum to PBS (pH?～?7.4) boosted the drug release. 5-FU-rHSA-NPs and 5-FU-rHSA-PEG-NPs released 78.26% and 48.9% of the 5-FU up to 48?h in presence of PBS (pH?～?7.4 and 20% serum) with significant difference (P?50 of 3.7-μM significantly (P?1/2) of 5.33?±?0.15-h significantly (P?a clinical product.
Electrophilic addition to the multiple bond of 1-carboxymethyl-5-fluorouracil
Chernikova, I. B.,Mustaphin, A. G.,Yunusov, M. S.
, p. 114 - 117 (2020)
1-Carboxymethyl-5-fluoro-5-halogeno-6-hydroxy-5,6-dihydrouracils and 1-carboxymethyl- 5-fluoro-6-hydroxy-5-nitro-5,6-dihydrouracil were synthesized in high yields by oxidative halogenation or nitration of 1-carboxymethyl-5-fluorouracil. Oxidative halogenation or nitration of 5-fluoro-1-(methoxycarbonylmethyl)uracil in acidic media results in the addition of the corresponding groups at the C(5) atom of uracil and simultaneous hydrolysis of the ester group. Bimolecular ions of the obtained compounds were detected in the negative ion mass spectra.
