Cytosine analogue, process for the preparation of cytosine analogue, DNA methyltransferase 1 inhibitor, method for DNA methylation inhibition, the use of analog in the treatment of diseases involving deviations from the standard DNA methylation
INSTYTUT CHEMII BIOORGANICZNEJ POLSKIEJ AKADEMII NAUK
发明人:
BARCISZEWSKI, JAN,JAN BARCISZEWSKI,MARKIEWICZ, WOJCIECH T.,WOJCIECH T. MARKIEWICZ,ADAMSKA, EWELINA,EWELINA ADAMSKA,PLITTA, BEATA,BEATA PLITTA,GIEL-PIETRASZUK, MAŁGORZATA,MAŁGORZATA GIEL-PIETRASZUK,WYS,ELI
申请号：
PL390769
公开号：
PL229581B1
申请日:
2010.03.19
申请国别(地区):
PL
年份:
2018
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 formula where R1 is H, R3, R4, 2&prime；-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.
