- Synthesis and crystallographic analysis of short pyridine-based oligoamides as DNA-targeting supramolecular binders
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In this study, the synthesis of the pyridine peptides 1-4, formed from amino-picolinic acid, and pyridine peptide 5, made from coupling of a mono-protected pyridine diamine to a mono-protected pyridine dicarboxylic acid and the X-ray crystallographic structures of 1 and 5 are discussed, along with their supramolecular interactions in the solid state. The structure of these compounds showed that they possess concave appearance which can be employed to bind to nucleic acids through multiple hydrogen bonding, which would facilitate the formation of helical-based pyridine oligoamides as novel DNA-binding molecules. This was proven by carrying out DNA denaturation studies and ethidium displacement assay on 5, but, by using MTT assays, 5 was shown to be cytotoxic against drug-resistant chronic myeloid leukaemia K562 cell-line.
- Frimannsson, Daniel O.,McCabe, Thomas,Schmitt, Wolfgang,Lawler, Mark,Gunnlaugsson, Thorfinnur
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- Hydrogen bonding control of molecular self-assembly: Aggregation behavior of acylaminopyridine-carboxylic acid derivatives in solution and the solid state
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In this paper we report the design, synthesis and investigation of a family of acylaminopyridine-carboxylic acid monomers that can aggregate through bidentate hydrogen bonding interactions between the carboxylic acid and the aminopyridine sites. We show that in solution the nature of the aggregate depends on the substitution pattern of the monomer and present evidence from NMR and mass spectrometry that in some cases cyclic association occurs. (C) 2000 Elsevier Science Ltd.
- Zafar, Abdullah,Geib, Steven J.,Hamuro, Yoshitomo,Carr, Andrew J.,Hamilton, Andrew D.
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- DIHYDROPYRIDAZINONES SUBSTITUTED WITH PHENYLUREAS
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Compounds of formula (I) which are nicotinamide phosphoribosyltransferase (NAMPT) inhibitors and their use for the treatment of hyperproloferative diseases and/or disorders responsive to induction of cell death.
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(2018/05/27)
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- INDOLYLMETHYL-MORPHOLINE DERIVATIVES AS KINASE INHIBITORS
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A series of morpholine derivatives, substituted in the 4-position by a substituted carbonyl or sulfonyl moiety, and in the 3-position by an optionally substituted indol-3-ylmethyl group, being selective inhibitors of PI3 kinase enzymes, are accordingly of
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Page/Page column 43
(2010/12/31)
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- INHIBITORS OF HISTONE DEACETYLASE
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The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
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Page/Page column 221
(2010/02/11)
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- FUSED AZOLE-PYRIMIDINE DERIVATIVES
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The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidy
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