Tezacitabine
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Tezacitabine
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CAS No:
130306-02-4
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Formula:
C10H12FN3O4
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Chemical Name:
Tezacitabine
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Synonyms:
Cytidine,2′-deoxy-2′-(fluoromethylene)-,(2′E)-;(2′E)-2′-Deoxy-2′-(fluoromethylene)cytidine;(E)-2′-Deoxy-2′-(fluoromethylene)cytidine;MDL 101731;FMdC;Tezacitabine;KW 2331
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CAS No:
Description
A synthetic purine nucleoside analogue with potential antineoplastic activity.|Tezacitabine Anhydrous is the anhydrous form of tezacitabine, a synthetic pyrimidine nucleoside analogue with potential antineoplastic activity. Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites. Tezacitabine diphosphate binds to and irreversibly inhibits the activity of the enzyme ribonucleotide reductase (RNR), which may result in the inhibition of DNA synthesis in tumor cells and eventually tumor cell apoptosis. Tezacitabine triphosphate acts as a substrate for DNA polymerase, thereby further inhibiting DNA replication. RNR catalyzes the conversion of ribonucleoside 5'-diphosphates to deoxyribonucleoside 5'-diphosphates, a necessary step for DNA synthesis, and is overexpressed in many tumor cell types.
Drug Information
Investigated for use/treatment in colorectal cancer, lung cancer, leukemia (unspecified), and gastric cancer.
Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)|Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. (See all compounds classified as Enzyme Inhibitors.)|Drugs used to potentiate the effectiveness of radiation therapy in destroying unwanted cells. (See all compounds classified as Radiation-Sensitizing Agents.)
Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites. Tezacitabine diphosphate binds to and irreversibly inhibits the activity of the enzyme ribonucleotide reductase (RNR), which may result in the inhibition of DNA synthesis in tumor cells and tumor cell apoptosis. Tezacitabine triphosphate acts as a substrate for DNA polymerase, further compromising DNA replication. This agent is relatively resistant to metabolic deactivation by cytidine deaminase. RNR catalyzes the conversion of ribonucleoside 5'-diphosphates to deoxyribonucleoside 5'-diphosphates necessary for DNA synthesis and is overexpressed in many tumor types.
2'-deoxy-2'-(fluoromethylene)cytidine
Computed Properties
Molecular Weight:257.22
XLogP3:-2.3
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:2
Exact Mass:257.08118403
Monoisotopic Mass:257.08118403
Topological Polar Surface Area:108
Heavy Atom Count:18
Complexity:448
Defined Atom Stereocenter Count:3
Defined Bond Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes
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