1320288-24-1

Upstream product

• 19748-66-4 3-pyrrolidin-1-yl-propan-1-ol 
• 214470-57-2 methyl 4-(3-chloropropoxy)-5-methoxy-2-nitrobenzoate 
• 111627-40-8 methyl 4-(3-chloropropoxy)-3-methoxybenzoate 
• 3943-74-6 4-hydroxy-3-methoxybenzoic acid methyl ester 
• 1320288-23-0 methyl 5-methoxy-2-nitro-4-[3-(pyrrolidin-1-yl)propoxy]benzoate 

Downstream Products

• 1320288-30-9 2,4-dichloro-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline 
• 1320288-52-5 2-(4-cyclohexyl-1,4-diazepan-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine 
• 1320288-54-7 2-(4-(cyclohexylmethyl)-1,4-diazepan-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine 
• 1320288-56-9 N-(1-isopropylpiperidin-4-yl)-6-methoxy-2-(4-phenyl-1,4-diazepan-1-yl)-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine 
• 1320288-58-1 2-(4-benzyl-1,4-diazepan-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine 
• 1320288-29-6 6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)-1H-quinazoline-2,4-dione 
• 1481677-78-4 UNC0642 
• 1586014-83-6 2-cyclohexyl-N-(1-(hex-5-yn-1-yl)piperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine 
• 1327276-41-4 C₂₂H₃₀ClN₃O₂ 
• 1586020-01-0 N-(2-(2-(2-(2-(4-(4-(4-((2-cyclohexyl-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-yl)amino)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide 

Relevant academic research and scientific papers

TRICYCLIC COMPOUNDS AS HISTONE METHYLTRANSFERASE INHIBITORS

The present disclosure provides tricyclic compounds of formula (I) that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobi

NOVEL COMPOUNDS AS INHIBITORS OF DNA METHYLTRANSFERASES

It relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein A, R1, R2, and R3 are as defined herein, which are inhibitors of one or more DNMTs selected from the group consisting of DNMT1, DNMT3A and DNMT3B. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of cancer, fibrosis and/or immunomodulation.

HISTONE METHYLTRANSFERASE INHIBITORS

The present disclosure provides certain compounds of formula (I) that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinpathies such as beta-thalassemia and sickle cell disease. Also provided are pharmaceutical compositions containing such compounds as well as processes and intermediates for preparing such compounds.

A chemical tool for in vitro and in vivo precipitation of lysine methyltransferase G9a

Here we report the design, synthesis, and biochemical characterization of a new chemical tool, UNC0965. UNC0965 is a biotinylated version of our previously reported G9a chemical probe, UNC0638. Importantly, UNC0965 maintains high in vitro potency and is c

Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP

Among epigenetic "writers", "readers", and "erasers", the lysine methyltransferases G9a and GLP, which catalyze mono- and dimethylation of histone H3 lysine 9 (H3K9me2) and nonhistone proteins, have been implicated in a variety of human diseases. A "toolk

Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy- quinazolines

Protein lysine methyltransferase G9a plays key roles in the transcriptional repression of a variety of genes via dimethylation of lysine 9 on histone H3 (H3K9me2) of chromatin as well as dimethylation of nonhistone proteins including tumor suppressor p53. We previously reported the discovery of UNC0321 (3), the most potent G9a inhibitor to date, via structure-based design and structure-activity relationship (SAR) exploration of the quinazoline scaffold represented by BIX01294 (1). Despite its very high in vitro potency, compound 3 lacks sufficient cellular potency. The design and synthesis of several generations of new analogues aimed at improving cell membrane permeability while maintaining high in vitro potency resulted in the discovery of a number of novel G9a inhibitors such as UNC0646 (6) and UNC0631 (7) with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity. The design, synthesis, and cellular SAR of these potent G9a inhibitors are described.