Abstract：
:2'-Deoxy-N4-[2-(4-nitrophenyl)ethoxycarbonyl]-5-azacytidine (NPEOC-DAC), decitabine with a modification of the N4 position of the azacitidine ring can be used to inhibit DNA methyltransferase. This modification protects the azacitidine ring and can be cleaved by carboxylesterase to release decitabine. NPEOC-DAC was 23-fold less potent at low doses (<10microM) than decitabine at inhibiting DNA methylation, and was also associated with a 3-day delay in its effect. However, at doses > or = 10microM NPEOC-DAC was more effective at inhibiting DNA methylation. Theses differences between decitabine and NPEOC-DAC are dependent on the cleavage of the carboxylester bond, and could be potentially exploited pharmacologically.
journal_name
Cancer Lettjournal_title
Cancer lettersauthors
Byun HM,Choi SH,Laird PW,Trinh B,Siddiqui MA,Marquez VE,Yang ASdoi
10.1016/j.canlet.2008.02.069subject
Has Abstractpub_date
2008-08-08 00:00:00pages
238-48issue
2eissn
0304-3835issn
1872-7980pii
S0304-3835(08)00171-7journal_volume
266pub_type
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