1101181-35-4Relevant academic research and scientific papers
Total synthesis and biological evaluation of tubulysin U, tubulysin V, and their analogues
Balasubramanian, Ranganathan,Raghavan, Bhooma,Begaye, Adrian,Sackett, Dan L.,Fecik, Robert A.
supporting information; experimental part, p. 238 - 240 (2009/09/25)
A stereoselective total synthesis of the cytotoxic natural products tubulysin U, tubulysin V, and its unnatural epimer epitubulysin V, is reported. Simplified analogues containing N,N-dimethyl- D-alanine as a replacement for the N-terminal N-Me-pipecolinic acid residue of the tubulysins are also disclosed. Biological evaluation of these natural products and analogues provided key information with regard to structural and stereochemical requirements for antiproliferative activity and tubulin polymerization inhibition.
