128550-06-1Relevant articles and documents
Homologation of polyamines in the synthesis of lipo-spermine conjugates and related lipoplexes
Geall, Andrew J.,Blagbrough, Ian S.
, p. 443 - 446 (1998)
Polyamine amides are useful in gene delivery as synthetic (non-viral) vectors or mimics of polycationic histones. The application of a homologation strategy, based upon reductive alkylation, allows unsymmetrical polyamine amides to be prepared in good yie
NEW (POLY)AMINOALKYLAMINOALKYLAMIDE, ALKYL-UREA, OR ALKYL-SULFONAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN, A PROCESS FOR PREPARING THEM, AND APPLICATION THEREOF IN THERAPY AS ANTICANCER AGENTS
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Page/Page column 51, (2010/04/03)
The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamidc, or alkyl-urea or alkyl- sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: - R represents hydrogen or C1-4alkyI, - A represents CO(CH2)n or CONH(CH2)n where n = 2, 3, 4, or 5, - R1 and R2 are as described herein.
Polycationic sulfonamides for the sequestration of endotoxin
Burns, Mark R.,Jenkins, Scott A.,Kimbrell, Matthew R.,Balakrishna, Rajalakshmi,Nguyen, Thuan B.,Abbo, Benjamin G.,David, Sunil A.
, p. 877 - 888 (2007/10/03)
Lipopolysaccharides (LPS) play a key role in the pathogenesis of septic shock, a major cause of mortality in the critically ill patient. We had previously shown that monoacylated polyamine compounds specifically bind to and neutralize the activity of LPS with high in vitro potency and afford complete protection in a murine model of endotoxic shock. Fatty acid amides of polyamines may be rapidly cleared from systemic circulation due to their susceptibility to nonspecific serum amidases and, thus, would be predicted to have a short duration of action. In a systematic effort to increase the likelihood of better bioavailability properties together with structural modifications that may result in gains in activity, we now report structure-activity relationships pertaining to endotoxin-binding and -neutralizing activities of homologated polyamine sulfonamides.