Issue 9, 2012

A straightforward click-approach towards pretubulysin-analogues

Abstract

The [3+2]-cycloaddition of an azido tripeptide, corresponding to the left hand side of pretubulysin, with a range of alkynes, such as propiolic acid amides and propargyl ethers, allows the straightforward syntheses of libraries of tubulysin derivatives. Via this click approach, a chimera of pretubulysin and dolastatin 10, both highly potent antimitotic drug candidates, also becomes accessible.

Graphical abstract: A straightforward click-approach towards pretubulysin-analogues

Supplementary files

Article information

Article type
Paper
Submitted
02 Feb 2012
Accepted
06 Feb 2012
First published
07 Mar 2012

RSC Adv., 2012,2, 3785-3790

A straightforward click-approach towards pretubulysin-analogues

J. L. Burkhart and U. Kazmaier, RSC Adv., 2012, 2, 3785 DOI: 10.1039/C2RA20191G

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