475272-69-6

Upstream product

• 16013-85-7 2,6-dicholoro-3-nitropyridine 
• 186413-90-1 6-isopropoxy-5-nitropyridine-2-carboxylic acid 
• 186413-80-9 2-isopropoxy-3-nitro-6-vinylpyridine 
• 186413-77-4 6-chloro-3-nitro-2-(propan-2-yloxy)pyridine 
• 92138-35-7 6-chloro-3-nitro-1H-pyridin-2-one 
• 475272-66-3 Methyl 6-isopropoxy-5-nitro-2-pyridinecarboxylate 

Downstream Products

• 475272-83-4 5-[(6-benzyloxy-5-nitro-pyridine-2-carbonyl)-amino]-6-isopropoxy-pyridine-2-carboxylic acid methyl ester 
• 1373319-36-8 5-(5-(4-amino-3-isopropoxybenzamido)-6-isopropoxypicolinamido)-6-isopropoxypicolinic acid 
• 1373319-48-2 methyl 5-(5-(4-amino-3-isopropoxybenzamido)-6-isopropoxypicolinamido)-6-isopropoxypicolinate 
• 1373319-44-8 methyl 6-isopropoxy-5-(6-isopropoxy-5-(3-isopropoxy-4-nitrobenzamido)picolinamido)picolinate 
• 475272-87-8 Methyl 5-{[(6-(benzyloxy)-5-{[(6-isopropoxy-5-nitro-2-pyridinyl)carbonyl]amino}-2-pyridinyl)carbonyl]amino}-6-isopropoxy-2-pyridine carboxylate 
• 475272-74-3 Methyl 5-{[(5-amino-6-(benzyloxy)-2-pyridinyl)carbonyl]amino}-6-isopropoxy-2-pyridinecarboxylate 

Relevant academic research and scientific papers

Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: Identification of potent Bcl-xL inhibitors

By conducting a structure-activity relationship study of the backbone of a series of oligoamide-foldamer-based α-helix mimetics of the Bak BH3 helix, we have identified especially potent inhibitors of Bcl-xL. The most potent compound has a Ki value of 94 nM in vitro, and single-digit micromolar IC50 values against the proliferation of several Bcl-xL-overexpressing cancer cell lines. The Royal Society of Chemistry 2012.

Design and application of an α-helix-mimetic scaffold based on an oligoamide-foldamer strategy: Antagonism of the Bak BH3/Bcl-xL complex

The prevention of cell death by the antiapoptotic protein Bcl-xL has been linked to a number of cancers. Bcl-xl binds to the BH3 domain of the proapoptotic protein Bak, thus preventing programmed cell death. A competitive assay and docking studies have shown that the polyamide scaffold 1, which was synthesized based on a rational structure-based design, interferes with the Bak BH3/Bcl-xl complexation.

Proteomimetic compounds and methods

The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.