Phorboxazole analogues induce association of cdk4 with extranuclear cytokeratin intermediate filaments
The cellular localization profile and molecular association of the phorboxazoles were examined with a streamlined target elucidation system using synthetic fluorescent probes. Cellular image analyses identified the binding of phorboxazole analogues to cyt
Forsyth, Craig J.,Ying, Lu,Chen, Jiehao,La Clair, James J.
GALNAC PHOSPHORAMIDITES, NUCLEIC ACID CONJUGATES THEREOF AND THEIR USE
This invention generally relates to the field of phosphoramidite derivatives. In particular, the invention relates to N-Acetylgalactosamine phosphoramidite molecules and to conjugates of nucleic acid molecules with N-Acetylgalactosamine containing molecules. Also provided are methods for preparation of these molecules and possible uses thereof, in particular in medicine.
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Page/Page column 62
(2016/05/02)
[...] derivative compounds
PROBLEM TO BE SOLVED: To provide compounds improved in specific accumulation in amyloid deposition sites.SOLUTION: There are provided styrylpyridine derivative compounds represented by a prescribed general formula or salts thereof, and pharmaceutical comp
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Paragraph 0046-0049
(2020/02/10)
Synthesis of atorvastatin lactone linker constructs for target fishing
With the aim of connecting atorvastatin lactone 9 to a linker for affinity-based target fishing, a concise route to the pyrrolecarboxylic acid 8 was developed. Key features of the synthesis of the diol-containing side-chain were a catalytic enantioselecti
Sawant, Pramod,Maier, Martin E.
p. 6576 - 6585
(2013/01/15)
Synthesis of a heterobifunctional PEG spacer terminated with aminooxy and bromide functionality
A simple and efficient synthesis of a novel heterobifunctional polyethylene glycol (PEG) spacer is described. The PEG spacer reagent is terminated with aminooxy and bromide functionality for ease of conjugation to a variety of electrophiles and/or nucleop
Dicus, Christopher W.,Nantz, Michael H.
p. 2821 - 2823
(2008/02/11)
Design and total synthesis of a fluorescent phorboxazole a analog for cellular studies
To enable studies to elucidate the intracellular processing and targeting of the potent cytostatic/apoptotic anticancer natural products phorboxazoles A and B, a fluorescent derivative has been developed. This involved the total syntheses of the terminal
Chen, Jiehao,Ying, Lu,Hansen, T. Matthew,Engler, Mary M.,Lee, Chi Sing,La Clair, James J.,Forsyth, Craig J.
p. 901 - 904
(2007/10/03)
Vinyl Epoxides: Reagents for Radical-Induced DNA Cleavage
Allyloxyl radicals, formed by addition of thiyl radicals to vinyl epoxides, function as DNA-cleaving agents.Radical-induced damage to DNA is normally caused either by hydrogen-atom abstraction from deoxyribose or addition to the ?-bonds of the heterocyclic bases.Model studies showed that allyloxyl radicals could effect both hydrogen-atom abstraction and addition to simple alkene ?-bonds (but no product of addition to the ?-bonds of adenine was observed).Importantly, this model chemistry could be performed in water at room temperature, and using enzymic formation of glutathionyl radicals.An intercalating vinyl epoxide 35 bound to ΦX174 supercoited DNA caused cleavage when activated by glutathionyl radicals.The potential use of epoxide 35 in reversing the radiation resistance of tumours with a high local concentration of glutathione is discussed.
Breen, Anthony P.,Murphy, John A.
p. 2979 - 2990
(2007/10/02)
Modelling Radical-initiated DNA Cleavage by Vinyl Epoxides
Allyloxy radicals, formed by addition of thio radicals to vinyl epoxides, are shown to abstract hydrogen atoms and to add to alkene ?-bonds in reactions which model the chemistry that would be required to induce DNA damage; this suggests that vinyl epoxides could have uses as radiosensitizers for treatment of resistant tumours.
Breen, Anthony P.,Murphy, John A.
p. 191 - 192
(2007/10/02)
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