Structure-activity and high-content imaging analyses of novel tubulysins

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journalpeer-review

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Author(s)

  • Zhiyong Wang
  • Peter A. McPherson
  • Brianne S. Raccor
  • Raghavan Balachandran
  • Billy W. Day
  • Andreas Vogt
  • Peter Wipf

Detail(s)

Original languageEnglish
Pages (from-to)75-86
Journal / PublicationChemical Biology and Drug Design
Volume70
Issue number2
Publication statusPublished - Aug 2007
Externally publishedYes

Abstract

The synthesis and biological evaluation of three tubulysin analogs provides the first structure-activity relationship in this family of potent cytotoxic myxobacteria metabolites. Most importantly, the labile N,O-acetal at N 14 is not essential for biological activity. Further, structural simplifications are possible without abolishing biological activities. The N-terminal amino acid can be replaced with N-methylsarcosine, and the configuration at the acetoxy-bearing stereocenter at C11 is important but not critical for almost all aspects of the biological profile. Our data encourage further development of these compounds as potential therapeutic agents in cancer treatment. © 2007 The Authors.

Research Area(s)

  • Anticancer agent, Antimitotic, Chemical analogs, Cytotoxicity, Natural products, Structure-activity relationship, Tubulin, Tubulysin

Citation Format(s)

Structure-activity and high-content imaging analyses of novel tubulysins. / Wang, Zhiyong; McPherson, Peter A.; Raccor, Brianne S.; Balachandran, Raghavan; Zhu, Guangyu; Day, Billy W.; Vogt, Andreas; Wipf, Peter.

In: Chemical Biology and Drug Design, Vol. 70, No. 2, 08.2007, p. 75-86.

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journalpeer-review