Author/Authors :
Kenji Sugimoto، نويسنده , , Yuta Kobayashi، نويسنده , , Ayana Hori، نويسنده , , Takashi Kondo، نويسنده , , Naoki Toyooka، نويسنده , , Hideo Nemoto، نويسنده , , Yuji Matsuya، نويسنده ,
Abstract :
Syntheses of 16-membered macrolactams, which were aza-analogues of macrosphelides, could be established effectively by a ring-closing metathesis (RCM) strategy. Novel 19 analogues and six aza-macrosphelide–epothilone hybrids were furnished according to simple operations. Biological assay of these artificial aza-macrosphelides revealed that some of them showed stronger apoptosis-inducing activity against human lymphoma cells than the parent compound.
Keywords :
RCM strategy , Aza-analogue , Apoptosis-inducing activity , Macrosphelide