5 fluorouracil

5-Fluorouracil (5-FU) is a uracil analog, an inhibitor of DNA synthesis. 5-Fluorouracil has antitumor activity and affects pyrimidine synthesis through inhibition of thymidylate synthase. 5-Fluorouracil causes apoptosis and autophagy.

1-Acetyl-3-o-toluyl-5-fluorouracil is a potent antineoplastic agent.

5-Fluorouracil-13C,15N2 is intended for use as an internal standard for the quantification of 5-flurouracil by GC- or LC-MS. 5-Fluorouracil is a pyrimidine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis. Intracellular metabolites of 5-fluorouracil exert cytotoxic effects by either inhibiting thymidylate synthetase, or through incorporation into RNA and DNA, ultimately initiating apoptosis.

5-Fluorouracil-1-yl acetic acid methyl ester is a PNA-related Derivative.

5-Fluorouracil-1-yl acetic acid is a PNA-related Derivative.

1-(b-D-Xylofuranosyl)-5-fluorouracil is a Nucleoside Derivative - Xylo-nucleoside, Fluoro-modified nucleoside, 5-Modified pyrimidine nucleoside.

5,6-dihydro-5-Fluorouracil (5-FUH2) is an inactive metabolite of 5-FU and can be used for the study of organismal metabolism.

Floxuridine (FUDR) is an antimetabolite, floxuridine inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity.

ZX-J-19J (N-(2,3-Diphenyl-6-quinoxalinyl)octanamide), an inhibitor of Cyclophilin J (CyPJ), demonstrates remarkable inhibition of tumor cell growth, comparable to cyclosporine A but much stronger than 5-fluorouracil.

Emitefur (BOF-A 2) is an orally active and potent 5-fluorouracil derivative with anticancer and antitumor activity.Emitefur is used in advanced gastric cancer, breast cancer and metabolism-related diseases.

1. Cinnamaldehyde (Cinnamic Aldehyde) has antipyretic activity. 2. Cinnamaldehyde is a sedative agent. 3. Cinnamaldehyde inhibits invasive capabilities of MDA-MB-435S cells was correlated with down-regulating the expression of miR-27a. 4. Cinnamaldehyde induces the generation of reactive oxygen species and exerts vasodilator and anticancer effects. 5. Cinnamaldehyde appears to be a promising candidate as an adjuvant in combination therapy with 5-fluorouracil (5-FU) and oxaliplatin (OXA), two chemotherapeutic agents used in CRC treatment. The possible mechanisms of its action may involve the regulation of drugmetabolizing genes. 6. Cinnamaldehyde plays a certain role in inhibiting the occurrence and progression of melanoma and its action mechanism may be manifested by inhibiting expression of VEGF and HIF-α, thus blood vessel simulation and formation of new blood vessels of melanoma cells, and growth of tumors accordingly.

5-fluorouridine is also known as FUrd, 5-Fluorouracil 1-beta-D-ribofuranoside, 5-Fur, or 5-Fluoro-uridine. 5-fluorouridine is a solid. This compound belongs to the pyrimidine nucleosides and analogues. These are compounds comprising a pyrimidine base attached to a sugar. 5-fluorouridine is known to target uridine phosphorylase. FUrd is often used in chemical and biochemical comparison studies with fluorouracil and thymine analogs.

Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. Carmofur has been known to induce leukoencephalopathy.

D-Ribofuranose 1-dihydrogen phosphate dicyclohexanamine, commonly referred to as ribose 1-phosphate, serves as a precursor in the synthesis of 5-fluorouracil (FUra) via uridine phosphorylase [1].

(E)-5-(2-Bromovinyl)uracil (BVU) is a pyrimidine base and an inactive metabolite of the antiviral agents sorivudine and (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) that may be regenerated to BVDU in vivo. BVU irreversibly inactivates dihydropyrimidine dehydrogenase (DPD) in an NADPH-dependent manner. It enhances the efficacy of the chemotherapeutic agent and DPD substrate 5-fluorouracil in a P388 murine leukemia model when administered at a dose of 200 μmol/kg, increasing survival time.

DSPE-PEG(2000)-amine is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-PE . It has been used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents.1,2,3DSPE-PEG(2000)-amine has also been used in the synthesis of fluorescein isothiocyanate-loaded mesoporous silica nanoparticles for imaging applications.4It can be conjugated to a variety of functional molecules for improved cellular targeting and uptake of DSPE-PEG(2000)-amine-containing nanoparticles.4,5 1.Sloat, B.R., Sandoval, M.A., Li, D., et al.In vitro and in vivo anti-tumor activities of a gemcitabine derivative carried by nanoparticlesInt. J. Pharm.409(1-2)278-288(2011) 2.Abd-Rabou, A.A., Bharali, D.J., and Mousa, S.A.Taribavirin and 5-fluorouracil-loaded pegylated-lipid nanoparticle synthesis, p38 docking, and antiproliferative effects on MCF-7 breast cancerPharm. Res.35(4)76(2018) 3.Affram, K., Udofot, O., Singh, M., et al.Smart thermosensitive liposomes for effective solid tumor therapy and in vivo imagingPLoS One12(9):e0815116(2017) 4.Wang, L.-S., Wu, L.-C., Lu, S.-Y., et al.Biofunctionalized phospholipid-capped mesoporous silica nanoshuttles for targeted drug delivery: Improved water suspensibility and decreased nonspecific protein bindingACS Nano4(8)4371-4379(2010) 5.Wen, X., Wang, K., Zhao, Z., et al.Brain-targeted delivery of trans-activating transcriptor-conjugated magnetic PLGA/lipid nanoparticlesPLoS One9(9):e106652(2014)

Ansatrienin B is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis., In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 21 nM), which is a measure of bone resorption, and pp60c-src kinase (IC50 = 50 nM). It is an inhibitor of translation at the protein synthesis stage by specific inhibition of L-leucine incorporation (IC50 = 58 nM in A549 cells). It also inhibits TNF-α-induced expression of intercellular adhesion molecule-1 (ICAM-1; IC50 = 300 nM). Early in vitro studies showed that ansatrienin B potentiates the chemotherapeutic action of 5-fluorouracil , cisplatin , bleomycin , mitomycin C , and 6-mercaptopurine. Ansatrienin B is a hydroquinone form of ansatrienin A .

Doxifluridine (AMC 0101) is a fluoropyrimidine derivative and oral prodrug of the antineoplastic agent 5-fluorouracil (5-FU) with antitumor activity. Doxifluridine, designed to circumvent the rapid degradation of 5-FU by dihydropyrimidine dehydrogenase in the gut wall, is converted into 5-FU in the presence of pyrimidine nucleoside phosphorylase. 5-FU interferes with DNA synthesis and subsequent cell division by reducing normal thymidine production and interferes with RNA transcription by competing with uridine triphosphate for incorporation into the RNA strand.

Fosifloxuridine nafalbenamide (NUC 3373), a pyrimidine nucleotide analogue, is a Thymidylate synthase inhibitor. NUC-3373 has anticancer activity. NUC-3373 is a ProTide transformation of 5-FU that generates much higher concentrations of FUDR-MP in patients' cells.

Capecitabine-d11 is a deuterated compound of Capecitabine. Capecitabine has a CAS number of 154361-50-9. Capecitabine is a fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand.

Edoxudine (Epoxudine), an antiviral drug, is an analogue of thymidine and shows effectiveness against the herpes simplex virus. Edoxudine is used as a 5-fluorouracil (FU) modulator. Edoxudine may be used to enhance the therapeutic index of 5-FU by reducing the catabolism, prolonging the plasma and intratumoral concentrations of 5-FU, and offering protection to normal organs by increasing the endogenous uridine levels. It can also enhance the antitumour action of 5-FU.

FOLFIRI Regimen is a chemotherapy regimen consisting of leucovorin calcium (calcium folinate), 5-fluorouracil, and irinotecan used during the treatment of advanced-stage and metastatic colorectal cancer.

Uridine triacetate (RG 2133 triacetate) (Tri-O-acetyl uridine), an orally active prodrug of uridine, is efficiently absorbed in the gut and swiftly deacetylated in the circulation to release free uridine. It is utilized in the research of 5-fluorouracil (5-FU) and capecitabine toxicity, particularly targeting early-onset cardiac or central nervous system (CNS) complications.

Sparfosate is a 5-fluorouracil biomodulator.

4-(3,4-Difluorobenzo)curcumin (CDF) is a semisynthetic coumarin noted for its antiparasitic and anticancer properties. It effectively reduces the population of Vero cells infected by T. gondii promastigotes and amastigotes, with EC50 values of 0.8 and 0.37 µM, respectively. Furthermore, at concentrations of 4 and 8 µM, CDF enhances the efficacy of 5-fluorouracil and oxaliplatin in inhibiting the formation of both primary and secondary colonospheres in chemoresistant HCT116 cells.

Ivaltinostat (CG-200745) formic is an oral active panHDAC inhibitor with an isohydroxamic acid component that binds zinc at the bottom of the catalytic pocket. Ivaltinostat formic inhibited the deacetylation of histone H3 and tubulin. Ivaltinostat formic promotes p53 accumulation, induces p53-dependent trans activation, and enhances MDM2 and p21 (Waf1/Cip1) protein expression. Ivaltinostat formic increases the sensitivity of Gemcitabine resistant cells to Gemcitabine and 5-Fluorouracil (5-FU). Ivaltinostat formic induces apoptosis and has antitumor effect.

Bis-Pro-5FU, a precursor to 5-Fluorouracil (5-FU), enhances the oral bioavailability and safety profile of 5-FU chemotherapy treatments. 5-FU itself is an antineoplastic antimetabolite extensively utilized in the research of colorectal and pancreatic cancer.

Nitrocaphane, in combination with 5-FU (fluorouracil), chemotherapy is considered as a protocol of choice in the treatment of malignant trophoblastic tumor.

Thymine is one of the four bases of DNA and is able to act as a target for 5-fluorouracil in animal cancer models with Km=2.3 μM.

Ureidopropionic acid (3-Ureidopropionic acid) is an intermediate in the metabolism of uracil. More specifically it is a breakdown product of dihydrouracil and is produced by the enzyme dihydropyrimidase. It is further decomposed to beta-alanine via the enzyme beta-ureidopropionase. Ureidopropionic acid is essentially a urea derivative of beta-alanine. High levels of Ureidopropionic acid are found in individuals with beta-ureidopropionase (UP) deficiency. Enzyme deficiencies in pyrimidine metabolism are associated with a risk for severe toxicity against the antineoplastic agent 5-fluorouracil.

6-Acetonyldihydrochelerythrine exhibits significant antioxidant activities, it exhibits significant anti-HIV activity in H9 lymphocytes with EC50 and TI (Therapeutic Index) values of 1.77 microg/mL and 14.6, respectively. 6-Acetonyldihydrochelerythrine is

6-Hydroxypyridin-2(1H)-one hydrochloride (2,6-Dihydroxypyridine hydrochloride) is used as a reagent to synthesize uridine phosphorylase inhibitors that increase Uridine (Urd) (U829910) levels. Uridine is a promising biochemical modulator to reduce 5-fluorouracil (5-FU) toxicity without impairing its antitumor activity.

Benzylacyclouridine (BAU) is a powerful and selective inhibitor of uridine phosphorylase, the initial enzyme involved in uridine catabolism. Additionally, it can regulate the cytotoxic adverse effects of 5-fluorouracil (5-FU) and its derivatives.

Eniluracil (GW776C85) is an orally activedihydropyrimidine dehydrogenase (DPD) inhibitor,increases the oral bioavailability of 5-FU to 100%, facilitating uniform absorption and predictable toxicity.

Ansatrienin A is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis. In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 64 nM), which is a measure of bone resorption, and pp60c-srcM kinase (IC50 = 100 nM). It also inhibits TNF-α-induced expression of intercellular adhesion molecule-1 (ICAM-1; IC50 = 570 nM). Early in vitro studies showed that ansatrienin A potentiates the chemotherapeutic action of 5-fluorouracil , cisplatin , bleomycin , mitomycin C , and 6-mercaptopurine. It is an oxidized form of ansatrienin B .

Capecitabine (Capecitibine) is a fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand.