158233-67-1Relevant articles and documents
Cytarabine derivatives, the preparation and use thereof
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, (2008/06/13)
Novel cytarabine derivatives of the formula STR1 where R1, R2 and R3, which can be identical or different, are each selected from the group consisting of hydrogen, aliphatic C2 -C5 -acyl, benzoyl or carboxy-C1 -C3 -alkylcarbonyl are described. The compounds are suitable for use directly or in the form of immunoliposomes for controlling diseases. Methods of preparing the novel cytarabine derivatives are also disclosed.
Synthesis of 4-Alkylcytosine Nucleosides and Evaluation of Cytostatic Activity in the L1210 Murine Leukemia
Schott, Herbert,Haeussler, Markus P.,Schwendener, Reto A.
, p. 465 - 470 (2007/10/02)
4-Alkylcytosine nucleosides 2 were prepared by nucleophilic substitution of the 4-(1,2,4-triazol-1-yl) residue of uracil nucleoside derivatives 1 using different amino compounds.The antitumor activity against L1210 murine leukemia of fifteen 4-alkylcytosine nucleosides dissolved in buffer or incorporated into liposomes was tested.Liposomal 1-(β-D-arabinofuranosyl)-4-octadecylamino-2(1H)-pyrimidinone (2d) having the highest activity gave an increase of life span (ILS) of 706percent and 6/6 survivors at 400 μmol/kg.The structurally related and well-known antitumor drug 1-(β-D-arabinofuranosyl)cytosine (araC) dissolved in buffer gave only 179percent ILS and 0/6 survivors under corresponding conditions.Derivatives 2a-c and 2e-f having shorter or longer alkyl chains were less active.All the other derivatives showed no antitumor effect.The activity of the 4-alkylcytosine nucleoside was also lost, when the arabinose residue was replaced by ribose or deoxyribose. - Key Words: Nucleosides / Murine leukemia / Liposomes / Leukemia / Cytosine / Antitumor agents / Carbohydrates