Synthesis, activity and metabolic stability of non-ribose containing inhibitors of histone methyltransferase DOT1L
Year: 2013
Type: article
Abstract: 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 ∼ 200 nM). Importantly, this compound exhibits a high stability in plasma and liver microsomes, suggesting it is a better drug candidate.
Source: MedChemComm
DOI: 10.1039/c3md00021d
Authors: Lisheng Deng, Li Zhang, Yuan Yao, Cong Wang, Michele S. Redell, Shuo Dong, Yongcheng Song
Institution: Baylor College of Medicine
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
Award: G5422687249
OpenAlex ID: W2057217306