%0 Journal Article
%@ 1747-0277
%A Wang, Z
%A McPherson, PA
%A Raccor, BS
%A Balachandran, R
%A Zhu, G
%A Day, BW
%A Vogt, A
%A Wipf, P
%D 2007
%F pittir:19461
%J Chemical Biology and Drug Design
%N 2
%P 75 - 86
%T Structure-activity and high-content imaging analyses of novel tubulysins
%U http://d-scholarship-dev.library.pitt.edu/19461/
%V 70
%X 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.