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

Wang, Z and McPherson, PA and Raccor, BS and Balachandran, R and Zhu, G and Day, BW and Vogt, A and Wipf, P (2007) Structure-activity and high-content imaging analyses of novel tubulysins. Chemical Biology and Drug Design, 70 (2). 75 - 86. ISSN 1747-0277

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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.


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Item Type: Article
Status: Published
CreatorsEmailPitt UsernameORCID
Wang, Z
McPherson, PA
Raccor, BS
Balachandran, R
Zhu, G
Day, BW
Vogt, A
Wipf, Ppwipf@pitt.eduPWIPF
Date: 1 August 2007
Date Type: Publication
Journal or Publication Title: Chemical Biology and Drug Design
Volume: 70
Number: 2
Page Range: 75 - 86
DOI or Unique Handle: 10.1111/j.1747-0285.2007.00541.x
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
ISSN: 1747-0277
MeSH Headings: Animals; Cattle; Cell Line, Tumor; Depsipeptides--metabolism; Glioblastoma--drug therapy; HeLa Cells; Humans; Mitosis--drug effects; Oligopeptides--chemical synthesis; Oligopeptides--chemistry; Oligopeptides--pharmacology; Oligopeptides--therapeutic use; Structure-Activity Relationship; Thiazoles--chemical synthesis; Thiazoles--chemistry; Thiazoles--therapeutic use; Tubulin--drug effects; Tubulin Modulators--pharmacology; Vinblastine--metabolism
PubMed ID: 17683369
Date Deposited: 07 Aug 2013 15:35
Last Modified: 12 Jun 2021 09:55


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