172992-25-5Relevant articles and documents
DNA condensation by cholesterol polyamine carbamates: A first step in gene therapy
Geall, Andrew J.,Blagbrough, Ian S.
, p. 145 - 150 (2007/10/03)
Novel cholesterol polyamine carbamates were prepared and their pKa values determined potentiometrically. Using the Henderson-Hasselbach equation, their charge, at physiological pH, was determined. Binding affinity for calf thymus DNA was measured using an
Practical synthesis of unsymmetrical polyamine amides
Blagbrough, Ian S.,Geall, Andrew J.
, p. 439 - 442 (2007/10/03)
Desymmetrisation of readily available symmetrical polyamines is an important first step in the synthesis of many polyamine containing natural products. Likewise in the synthesis of polyamine amides which are potentially useful for gene delivery and as neuroprotectants, based upon channel blocking toxins found in certain wasp and spider venoms. The application of trifluoroacetyl as a protecting group allows unsymmetrical polyamine amides to be easily prepared on a gram scale.
Inhibition of growth of B16 murine melanoma cells by novel spermine analogues
Carrington,Qarawi,Blagbrough,Moss,Pouton
, p. 25 - 27 (2007/10/03)
To develop new cytotoxins, which could find use as anti-cancer agents, polyamine conjugates were synthesized containing spermine and an anthracene or acridine unit. Spermine is known to groove-bind to DNA; anthracene and acridine are known to intercalate. It was hoped that these polyamine-polyaromatic conjugates would use both modes of binding. Studies of growth inhibition of B16 murine melanoma cells showed the conjuates to be more effective than either spermine, anthracene-9-carboxylic acid or acridine-9-carboxylic acid, and of the conjugates, the acridine derivative showed greatest activity.
Total Synthesis of Polyamine Amides PhTX-4.3.3 and PhTX-3.4.3: Reductive Alkylation is a Rapid, Practical Route to Philanthotoxins
Eduardo, Moya,Blagbrough, Ian S.
, p. 9401 - 9404 (2007/10/02)
Reductive alkylation allows a rapid and practical entry to the polyamine amide wasp toxin philanthotoxin-4.3.3.Philanthotoxin-3.4.3 has been prepared, in two steps, by the monoacylation of sperimine.These polyamine amides are selective molecular pharmacological tools for cation channels gated by glutamic acid and acetylcholine, and may have potential as a neuroprotective agents.
Total synthesis of modified JSTX toxins: Reductive alkylation is a practical route to hexahydropyrimidine polyamine amides
Ashton, Mark R.,Moya, Eduardo,Blagbroug, Ian S.
, p. 9397 - 9400 (2007/10/02)
Reductive alkylation is a practical route for a total synthesis of regioisomers of spider toxin JSTX-3, a polyamine amide which is a selective glutamate receptor antagonist and may have potential as a neuroprotective agent. The strategy is based upon a re