Synthesis and Profiling of Highly Selective Inhibitors of Methyltransferase DOT1L Based on Carbocyclic C-Nucleosides.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02228
Abstract: Histone methyltransferase DOT1L is an attractive therapeutic target for the treatment of hematological malignancies. Here, we report the design, synthesis, and profiling of new DOT1L inhibitors based on nonroutine carbocyclic C-nucleoside scaffolds. The experimentally observed… read more here.
Keywords: inhibitors methyltransferase; profiling highly; selective inhibitors; methyltransferase dot1l ... See more keywords
Synthesis and Profiling of a Novel Potent Selective Inhibitor of CHK1 Kinase Possessing Unusual N-trifluoromethylpyrazole Pharmacophore Resistant to Metabolic N-dealkylation
Sign Up to like & getrecommendations! Published in 2017 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.mct-17-0018
Abstract: Checkpoint-mediated dependency of tumor cells can be deployed to selectively kill them without substantial toxicity to normal cells. Specifically, loss of CHK1, a serine threonine kinase involved in the surveillance of the G2–M checkpoint in… read more here.
Keywords: dealkylation; chk1; synthesis profiling; unusual trifluoromethylpyrazole ... See more keywords