1020657-43-5Relevant articles and documents
SALT OF TRIPHOSPHATE PHOSPHORAMIDATES OF NUCLEOTIDES AS ANTICANCER COMPOUNDS
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Paragraph 00116, (2020/10/20)
The present invention relates to salts of triphosphate phosphoramidates which are useful in the treatment of cancer.
Efficient synthesis of gemcitabine 5′-O-triphosphate using gemcitabine 5′-O-phosphoramidate as an intermediate
Kaczmarek, Renata,Radzikowska, Ewa,Baraniak, Janina
supporting information, p. 1851 - 1854 (2014/08/18)
A new efficient approach for the synthesis of gemcitabine triphosphate has been developed. The method is based on the ring-opening reaction of 2-cyanoethoxy-2-oxo-1,3,2-oxathiaphospholane with protected gemcitabine in the presence of DBU. Subsequent treatment of gemcitabine monophosphate with DCC in the presence of ammonia provides gemcitabine 5′-O-phosphoramidate. Finally, this compound, on reaction with pyrophosphate, furnishes gemcitabine 5′-triphosphate in 50% yield. Georg Thieme Verlag Stuttgart. New York.
Syntheses of 5′-amino-2′,5′-dideoxy-2′,2′- difluorocytidine derivatives as novel anticancer nucleoside analogs
Labroli, Marc A.,Dwyer, Michael P.,Shen, Ruichao,Popovici-Muller, Janeta,Pu, Qinglin,Richard, Judson,Rosner, Kristen,Paruch, Kamil,Guzi, Timothy J.
, p. 598 - 602 (2014/01/23)
A novel class of 5′-amino-2′,5′-dideoxy-2′, 2′-difluorocytidine derivatives has been synthesized in order to identify anticancer nucleoside analogs. Several synthetic routes were devised and implemented which relied upon either SN2 displacement
The identification of novel 5′-amino gemcitabine analogs as potent RRM1 inhibitors
Labroli, Marc A.,Dwyer, Michael P.,Shen, Ruichao,Popovici-Muller, Janeta,Pu, Qinglin,Wyss, Daniel,McCoy, Mark,Barrett, Dianah,Davis, Nicole,Seghezzi, Wolfgang,Shanahan, Frances,Taricani, Lorena,Beaumont, Maribel,Malinao, Maria-Christina,Parry, David,Guzi, Timothy J.
, p. 2303 - 2310 (2014/04/17)
The ribonucleotide reductase (RNR) enzyme is a heteromer of RRM1 and RRM2 subunits. The active enzyme catalyzes de novo reduction of ribonucleotides to generate deoxyribonucleotides (dNTPs), which are required for DNA replication and DNA repair processes.
NOVEL MODULATORS OF CELL CYCLE CHECKPOINTS AND THEIR USE IN COMBINATION WITH CHECKPOINT KINASE INHIBITORS
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Page/Page column 83, (2009/06/27)
In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits