Synthesis and Evaluation of Hydroxylated Polyamine Analogues as Antiproliferatives
作者:Raymond J. Bergeron、Ralf Müller、Guangfei Huang、James S. McManis、Samuel E. Algee、Hua Yao、William R. Weimar、Jan Wiegand
DOI:10.1021/jm000532q
日期:2001.7.1
N(11)-diethyl-2,10-dihydroxynorspermine [(2S,10S)-(HO)(2)DENSPM] at 96 h. Both cyclopropyl compounds reduced putrescine and spermidine pools, but less effectively than did DENSPM and its derivatives. Only CPMENSPM, and not (2R,10S)-(HO)(2)CPMENSPM, lowered spermine pools. As with DENSPM and (2R,10R)-(HO)(2)DENSPM, both cyclopropyl analogues diminished ornithine decarboxylase and S-adenosylmethionine decarboxylase
一种访问N(1)-环丙基甲基-N(11)-乙基去甲精胺(CPMENSPM)的新方法和(2R,10S)-N(1)-环丙基甲基-2,10-二羟基-N(11)-的首次合成描述了乙基去甲精胺[(2R,10S)-(HO)(2)CPMENSPM]。与N(1),N(11)-diethylnorspermine(DENSPM)或(2R,10R)-N(1),N(11)-相比,这两种多胺类似物均对L1210鼠白血病细胞的生长更具活性。处理96小时后,生成2,10-二羟基去甲精胺二乙基[(2R,10R)-(HO)(2)DENSPM];在96小时时,该活性可与(2S,10S)-N(1),N(11)-二乙基-2,10-二羟基去甲精胺[(2S,10S)-(HO)(2)DENSPM]媲美。两种环丙基化合物都可以减少腐胺和亚精胺库,但效果不如DENSPM及其衍生物。仅CPMENSPM,而不是(2R,10S)-(HO)(2