1440510-02-0Relevant articles and documents
NON-RIBOSE CONTAINING INHIBITORS OF HISTONE METHYLTRANSFERASE DOT1L FOR CANCER TREATMENT
-
Paragraph 0062; 0063; 00118, (2015/02/19)
A compound of Formula I, a pharmaceutically acceptable salt thereof, a prodrug thereof, or combinations thereof: wherein R1 is H, methyl, or benzyl: R2 is 2-cyanoethyl, 2-methoxycarbonylethyl, or 2-iodoethyl; X is N or S; wherein if
Synthesis, activity and metabolic stability of non-ribose containing inhibitors of histone methyltransferase DOT1L
Deng, Lisheng,Zhang, Li,Yao, Yuan,Wang, Cong,Redell, Michele S.,Dong, Shuo,Song, Yongcheng
, p. 822 - 826 (2013/08/26)
Histone methyltransferase DOT1L is a drug target for MLL leukemia. We report an efficient synthesis of a cyclopentane-containing compound that potently and selectively inhibits DOT1L (Ki = 1.1 nM) as well as H3K79 methylation (IC50 ~