Tetrahedron

Syntheses of aza-analogues of macrosphelides via RCM strategy and their biological evaluation

K Sugimoto, Y Kobayashi, A Hori, T Kondo, N Toyooka…

Index: Sugimoto, Kenji; Kobayashi, Yuta; Hori, Ayana; Kondo, Takashi; Toyooka, Naoki; Nemoto, Hideo; Matsuya, Yuji Tetrahedron, 2011 , vol. 67, # 40 p. 7681 - 7685

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Citation Number: 6

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 ...