Search results for "5-Fluorouracil"
showing 8 items of 28 documents
Pharmacokinetic and metabolism determinants of fluoropyrimidines and oxaliplatin activity in treatment of colorectal patients
2011
Fluoropyrimidines and oxaliplatin continued to be the mainstay of therapeutic regimens in the treatment of colorectal cancer (CRC). For this reason, pharmacokinetic and metabolism of these drugs were analyzed and the identification of accurate and validated predictive, prognostic and toxicity markers became necessary to develop an effective therapy adapted to the patient's molecular profile, while minimizing life-threatening toxicities. In this review, we discuss literature data, defining predictive and prognostic markers actually identified in the treatment of CRC. We analyzed predictive markers of fluoropyrimidines effectiveness, principally for 5-Fluorouracil (5-FU) and also for oral flu…
Discovery of SI 1/20 and SI 1/22 as Mutual Prodrugs of 5-Fluorouracil and Imidazole-Based Heme Oxygenase 1 Inhibitor with Improved Cytotoxicity in DU…
2023
: In this work, we extend the concept of 5-fluorouracil/heme oxygenase 1 (5-FU/HO-1) inhibitor hybrid as an effective strategy for enhancing 5-FU-based anticancer therapies. For this purpose, we designed and synthesized new mutual prodrugs, named SI 1/20 and SI 1/22, in which the two active parent drugs (i. e., 5-FU and an imidazole-based HO-1 inhibitor) were connected through an easily cleavable succinic linker. Experimental hydrolysis rate, and in silico ADMET predictions were indicative of good drug-likeness and pharmacokinetic properties. Novel hybrids significantly reduced the viability of prostate DU145 cancer cells compared to the parent compounds 5-FU and HO-1 inhibitor administered…
Liposomes as nonspecific nanocarriers for 5-Fluorouracil in the presence of cyclodextrins
2021
Abstract 5-Fluorouracil (5-FU) is one of anticancer drugs with broad activity. Due to its severe side effects, recent studies concentrate on new ways of directed 5-FU delivery and its release in ill tissue. One of selective carriers could be cyclodextrins and liposomes. The combination of novel methods, leading to formation of inclusion complexes (IC) between host molecule of β-cyclodextrin (β-CD) or 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and 5-FU guest and its subsequent encapsulation in dipalmitoylphosphatidylcholine (DPPC) liposomes is studied experimentally in the present work. Several methods are applied to proof the encapsulation of the analysed drug and its release over time at 37 …
Analisi dei polimorfismi dei geni codificanti per l’enzima UDP-glucuronosiltrasferasi (UGT) e per l’enzima diidropirimidina deidrogenasi (DPD), corre…
2012
CCDC 236010: Experimental Crystal Structure Determination
2005
Related Article: E.Saniger, M.Diaz-Gavilan, B.Delgado, D.Choquesillo, J.M.Gonzalez-Perez, S.Aiello, M.A.Gallo, A.Espinosa, J.M.Campos|2004|Tetrahedron|60|11453|doi:10.1016/j.tet.2004.09.077
CCDC 2064123: Experimental Crystal Structure Determination
2021
Related Article: Verónica G. Vegas, Ana Latorre, María Luisa Marcos, Carlos J. Gómez-García, Óscar Castillo, Félix Zamora, Jacobo Gómez, José Martínez-Costas, Miguel Vázquez López, Álvaro Somoza, Pilar Amo-Ochoa|2021|ACS Applied Materials and Interfaces|13|31|doi:10.1021/acsami.1c11612
Analysis of the Thymidylate Synthase Gene Structure in Colorectal Cancer Patients and lts Possible Relation with the S-Fluorouracil Drug Response
2010
Thymidylate synthase (TS) catalyzes methylation of dUMP to dTMP and it is the target for the 5-Fluorouracil (5-FU) activity*. Barbour et al. showed that variant structural forms of TS in tumour cell lines confer resistance to fluoropyrimidines. We planned to perform the whole TS gene structure by means of sequencing techniques in human colorectal cancer (CRC) san-rples to try to identify the presence of any possible TS variant form that could be responsible of fluoropyrimidines drug resistance and of the worse prognosis. We performed the TS-DNA gene sequence in 68 CRC from patients of A, B, and C Dukes' stages and different histological grade, but we did not find any mutation in the TS-DNA …
Tworzenie kompleksów inkluzyjnych pomiędzy 5-fluorouracylem a β-cyklodekstrynami
2017
Celem przedstawionego opracowania jest omówienie najważniejszych zagadnień dotyczących chemioterapii z użyciem 5-fluorouracylu, jego metabolizmu oraz zagrożenia wynikające z leczenia tym chemioterapeutykiem. Poruszona została również kwestia możliwości ograniczenia toksyczności 5FU, przez zainkludowaniu go we wnętrzu molekuły β-cyklodekstryny. Przedstawiono również najważniejsze wyniki badań teoretycznych w których przedstawiono geometrię kompleksu inkluzyjnego 5FU⎼βCD. Struktura została zoptymalizowana na poziomie teorii funkcjonału gęstości (DFT) z użyciem metody B3LYP/6-31G. Wykazano istnienie przynajmniej jednego wiązania wodorowego pomiędzy grupą aminową 5FU, a grupą hydroksylową powie…