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Antitumor Compounds Based on a Natural Product Consensus Pharmacophore.

  作者 Lagisetti, Chandraiah;Pourpak, Alan;Jiang, Qin;Cui, Xiaoli;Goronga, Tinopiwa;Morris, Stephan W.;Webb, Thomas R.;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-19;  页码  6220-6224  
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[摘要](Biomolecules and Their Synthetic Analogs) Section We report the design and highly enantioselective synthesis of a potent analog of the spliceosome inhibitor FR901464, based on a non-natural product scaffold. The design of this compd. was facilitated by a pharmacophore hypothesis that assumed key interaction types that are common to FR901464 and an otherwise unrelated natural product (pladienolide). The synthesis allows for the prepn. of numerous novel analogs. We present results on the in vitro activity for the compds. I, II and III against several tumor cell lines.

 
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