Abstract:
:Cytarabine is a chemotherapeutic agent predominately used for the treatment of acute myeloid leukemia and lymphoblastic leukemia. Cytarabine is a polar nucleoside, has a short plasma half-life, and its use is associated with severe side effects. Fatty acyl derivatives of cytarabine were synthesized with the expectation to improve cellular uptake and generate derivatives with a longer duration of action. Multi-step protection and deprotection reactions of hydroxyl and amino groups and conjugation with a fatty acid (i.e., myristic acid and 12-thioethyldodecanoic acid) afforded 5'-O-substituted, 2'-O-substituted, and 2',5'-disubstituted fatty acyl derivatives of cytarabine. 2',5'-Dimyristoyl derivative of cytarabine was found to inhibit the growth of CCRF-CEM cells by approximately 76% at concentration of 1 microM after 96 h incubation.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Chhikara BS,Mandal D,Parang Kdoi
10.1016/j.ejmech.2010.07.024subject
Has Abstractpub_date
2010-10-01 00:00:00pages
4601-8issue
10eissn
0223-5234issn
1768-3254pii
S0223-5234(10)00504-0journal_volume
45pub_type
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