Literature DB >> 10841498

On the total synthesis and preliminary biological evaluations of 15(R) and 15(S) aza-dEpoB: a Mitsunobu inversion at C15 in pre-epothilone fragments.

S J Stachel1, M D Chappell, C B Lee, S J Danishefsky, T C Chou, L He, S B Horwitz.   

Abstract

[reaction-see text] The syntheses of two epothilone analogues, 15(S)-aza-12,13-desoxyepothilone B and the epimeric 15(R)-aza-12,13-desoxyepothilone B, are described. A Mitsunobu inversion was utilized for elaboration of pre-epothilone fragments to the corresponding macrolactam. Tubulin binding and cytotoxicity profiles of these analogues are presented.

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Year:  2000        PMID： 10841498     DOI： 10.1021/ol005932m

Source DB:  PubMed          Journal:  Org Lett        ISSN： 1523-7052            Impact factor:   6.005


  3 in total

1.  The synthesis, discovery, and development of a highly promising class of microtubule stabilization agents: curative effects of desoxyepothilones B and F against human tumor xenografts in nude mice.

Authors:  T C Chou; O A O'Connor; W P Tong; Y Guan; Z G Zhang; S J Stachel; C Lee; S J Danishefsky
Journal:  Proc Natl Acad Sci U S A       Date:  2001-07-03       Impact factor: 11.205

2.  Subcellular distribution of epothilones in human tumor cells.

Authors:  R B Lichtner; A Rotgeri; T Bunte; B Buchmann; J Hoffmann; W Schwede; W Skuballa; U Klar
Journal:  Proc Natl Acad Sci U S A       Date:  2001-09-18       Impact factor: 11.205

3.  Meayamycin inhibits pre-messenger RNA splicing and exhibits picomolar activity against multidrug-resistant cells.

Authors:  Brian J Albert; Peter A McPherson; Kristine O'Brien; Nancy L Czaicki; Vincent Destefino; Sami Osman; Miaosheng Li; Billy W Day; Paula J Grabowski; Melissa J Moore; Andreas Vogt; Kazunori Koide
Journal:  Mol Cancer Ther       Date:  2009-08-11       Impact factor: 6.261
  3 in total

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