Tìm theo
Eniluracil
Các tên gọi khác (3) :
  • 5-ethynyl-2,4(1H,3H)-Pyrimidinedione
  • 5-Ethynyluracil
  • Compound 776C
enzyme inhibitors, antineoplastics adjuncts
Thuốc Gốc
Small Molecule
CAS: 59989-18-3
CTHH: C6H4N2O2
PTK: 136.1082
Eniluracil, which was previously under development by GlaxoSmithKline (GSK), is being developed by Adherex to enhance the therapeutic value and effectiveness of 5-fluorouracil (5-FU), one of the world’s most widely-used oncology agents. 5-FU is widely used in the U.S. and is often first or second line therapy for a variety of cancers including colorectal, breast, gastric, head and neck, ovarian and basal cell cancer of the skin. Eniluracil could improve 5-FU by increasing its effectiveness, reducing its side effects and/or making it orally available. Eniluracil has received Orphan Drug status from the FDA for the treatment of hepatocellular cancer in combination with fluoropyrimidines (including 5-FU).
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6H4N2O2
Phân tử khối
136.1082
Monoisotopic mass
136.027277382
InChI
InChI=1S/C6H4N2O2/c1-2-4-3-7-6(10)8-5(4)9/h1,3H,(H2,7,8,9,10)
InChI Key
InChIKey=JOZGNYDSEBIJDH-UHFFFAOYSA-N
IUPAC Name
5-ethynyl-1,2,3,4-tetrahydropyrimidine-2,4-dione
Traditional IUPAC Name
5-ethynyl-1,3-dihydropyrimidine-2,4-dione
SMILES
O=C1NC=C(C#C)C(=O)N1
Độ hòa tan
2.54e-01 g/l
logP
-0.82
logS
-2.7
pKa (strongest acidic)
9.5
pKa (Strongest Basic)
-6.4
PSA
58.2 Å2
Refractivity
33.39 m3·mol-1
Polarizability
12.05 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Eniluracil is an orally active dihydropyrimidine dehydrogenase (DPD) inhibitor, designed to enhance activity of chemotaxic agents. It is under investigation by Adherex, under license from GlaxoSmithKline, for the treatment of cancer in combination with 5-fluorouracil (5-FU).
Cơ Chế Tác Dụng : Eniluracil, which was previously under development by GlaxoSmithKline (GSK), is being developed by Adherex to enhance the therapeutic value and effectiveness of 5-fluorouracil (5-FU), one of the world’s most widely-used oncology agents. 5-FU is widely used in the U.S. and is often first or second line therapy for a variety of cancers including colorectal, breast, gastric, head and neck, ovarian and basal cell cancer of the skin. Eniluracil could improve 5-FU by increasing its effectiveness, reducing its side effects and/or making it orally available. Eniluracil has received Orphan Drug status from the FDA for the treatment of hepatocellular cancer in combination with fluoropyrimidines (including 5-FU). Normally, 5-FU is rapidly broken down in the body by an enzyme known as dihydropyrimidine dehydrogenase (DPD). Eniluracil irreversibly inhibits DPD, thereby substantially slowing the breakdown of 5-FU and prolonging exposure of the tumor cells to the drug.
Chỉ Định : For the treatment of cancer in combination with 5-fluorouracil.
Liều Lượng & Cách Dùng : Solution - Intravenous
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB03516
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=43157
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=12014705
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03998
ChemSpider
http://www.chemspider.com/Chemical-Structure.39327.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50124202
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