Spermine analogues

For the sake of brevity, salient aspects of key structure-activity relationships in one homologous series of twelve mono- and bis-acyl homologated spermine analogues (Fig. 12.8) will be first discussed (Miller et al., 2005). We addressed two questions in this study (i) what is the optimal hydrophobic chain length for effective anti-endotoxic activity, (ii) are symmetrical bis-acyl spermines more effective than mono-acyl compounds We found that a carbon number of 14-16 is optimal in mono-acyl spermines (Fig. 12.9) which are, in general, as potent as... 

The phosphinic acid polyamine analogue 370 is reported to be an effective inhibitor of purified human spermidine/spermine-N I-acetyltransferase (SSAT) and is claimed to be only the second example of a functional, non-superinducing inhibitor of human SSAT. The long-chain phosphonate analogues 371 and 372 are reported to exhibit cytostatic activity in vitro " ... 

Belton, D. Patwardhan, S. V. Peny, C. C., Spermine, spermidine and their analogues generate tailored silicas. J. Mater. Chem. 2005, 15, (43), 4629-4638. 

Saab, N.H., West, E.E., Bieszk, N.C., Pteuss, C.V., Mank, A.R., Casero, R.A. Jr, and Woster, PJ. (1993) Synthesis and evaluation of unsymmetrically substituted polyamine analogues as modulators of human spermidine/spermine-lV -acetyltransferase (SSAT) and as potential antitumor agents. J. Med. Chem. 36 2998-3004. 

Wang Y, Xiao L, ThiagaUngam A, NeUdn BD, Casero RA Jr (1998) The identification of a cis-element and a trans-acting factor involved in the response to polyamines and polyamine analogues in the regulation of the human spermidine/spermine Nl-acetyltransferase gene transcription. J Biol... 

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