- Programmable oligomers targeting 5′-GGGG-3′ in the minor groove of DNA and NF-κB binding inhibition
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A series of hairpin oligomers containing benzimidazole (Bi) and imidazopyridine (Ip) rings were synthesized and screened to target 5′-WGGGGW-3′, a core sequence in the DNA-binding site of NF-κB, a prolific transcription factor important in biology and disease. Five Bi and Ip containing oligomers bound to the 5′-WGGGGW-3′ site with high affinity. One of the oligomers (Im-Im-Im-Im-γ-Py-Bi-Py-Bi-β-Dp) was able to inhibit DNA binding by the transcription factor NF-κB.
- Chenoweth, David M.,Poposki, Julie A.,Marques, Michael A.,Dervan, Peter B.
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- N-(2-formyl-1-methylimidazol-4-yl)-2,2-dimethylpropanamide: A versatile reagent for preparing imidazole-amine ligands with variable second-coordination spheres
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Two synthetic pathways to N-(2-formyl-1-methylimidazol-4-yl)-2,2- dimethylpropanamide from 1-methyl-2-carboxaldehyde are described. The reagent serves as a useful synthon for reductive amination reactions with primary and secondary amines in the presence
- Cheruzel, Lionel E.,Cui, Jinlan,Mashuta, Mark S.,Grapperhaus, Craig A.,Buchanan, Robert M.
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supporting information; experimental part
p. 4771 - 4774
(2011/10/05)
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- OLIGOHETEROAROMATIC LUMINISCENT ASSEMBLIES AS HIGH-AFFINITY DNA SEQUENCE-DIRECTED LIGANDS
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The present invention provides a novel class of oligoheteroaromatic assemblies with luminescence characteristics and composition based on integrated polyheterocyclic polyamide oligomers of multiple nitrogen-containing heteroaromatic of the general formula (I) This novel class of compounds of the present invention is capable of binding to targeted DNA sequence in the minor groove, and thus is useful for genomics applications. In particular, the compounds of the invention binds to the DNA at a binding stoichiometry of 2: 1 ternary complexation with very high affinity and sequence selectivity.
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Page/Page column 41; 80
(2010/11/27)
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- Benzimidazole derivatives
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Disclosed are compounds represented by the following chemical formula (I) and pharmacologically acceptable salts thereof which are novel compounds useful as anticancer agents, antiviral agents or antimicrobial agents. STR1
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- 2-Substituted-1-alkyl-nitroimidazoles
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Novel 2-substituted 1-alkyl-nitroimidazoles and a process for their preparation by reaction of 2-methyl-nitroimidazoles with oxalic acid diesters, followed by reaction of the resulting nitroimidazol-2-yl-pyruvic acid esters with chlorine, in turn followed, if desired, by reaction of the resulting 2-dihalomethyl-nitroimidazoles with water. Both the novel and the known compounds obtainable by the process of the invention are valuable starting materials for the preparation of dyes, pesticides and drugs.
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