Cytosine analogue, a method of preparation of a cytosine analogue, a DNA methyltransferase 1 inhibitor, a method for DNA methylation inhibition, the use of the analogue in the treatment of diseases associated with deviations from normal DNA methylation
Jan Barciszewski,Wojciech T. Markiewicz,Ewelina Adamska,Beata Plitta,Malgorzata Giel-Pietraszuk,Eliza Wyszko,Maria Markiewicz,Agnieszka Fedoruk-Wyszomirska,Tadeusz Kulinski,Marcin Chmielewski
申请号：
US13576709
公开号：
US09040490B2
申请日:
2011.03.17
申请国别(地区):
US
年份:
2015
代理人:
摘要：
A cytosine analog, a method of preparation of a cytosine analog, a DNA methyltransferase 1 inhibitor, and a method for DNA methylation inhibition, is provided for the treatment of diseases associated with deviations from normal DNA methylation. The analog of cytosine may be comprised of 1, N4, 5 and 6-substituted derivatives of cytosine or 5,6-dihydrocytosine, wherein the analog can be described by the chemical formulawhere R1 is H, R3, R4, 2′-deoxyribosyl, R4 is alkyl or aryl, X is N or C, wherein if X in the analog of formula I is N, then R5 is no substituent and if X in the analog of formula I and/or II is C or if X in the analog of formula II is N, then R5 and R6 are independently alkyl, aryl, hydroxyalkyl, aminoalkyl, hydroxyl, carboxyl, amino group, alkoxyl, aryloxyl, aminoalkyl, aminoaryl, thio group, sulfonyl, sulfinyl or halogen.
