Synthesis, activity and metabolic stability of non-ribose containing inhibitors of histone methyltransferase DOT1L
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 ~
Synthesis of (-)-neplanocin A with the highest overall yield via an efficient Mitsunobu coupling
Neplanocin A was synthesized in very high isolated yield and purity, in 10 steps from d-ribose via an efficient Mitsunobu coupling using N6-bis-Boc-protected adenine. In fact, this synthesis is a short pathway to enantiopure neplanocin A giving
Michel, Beno?t Y.,Strazewski, Peter
p. 9836 - 9841
(2008/02/11)
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