Full text loading...
-
Recent Advances in the Synthesis of Tubulysins
- Source: Mini Reviews in Medicinal Chemistry, Volume 13, Issue 11, Oct 2013, p. 1572 - 1578
-
- 01 Oct 2013
Abstract
Tubulysins are a family of natural tetrapeptides in clinical development as a consequence of their potent anticancer activity, even for multi-drug resistant carcinoma. Tubulysins inhibit tubulin polymerization by binding to the peptide binding site located near the vinca alkaloid binding site of tubulin. The limited availability and pharmacological profile of the tubulysins attracted synthetic and medicinal chemists to initiate programs towards their total synthesis. This paper reviews efforts toward the total synthesis of tubulysins and selected structure-activity relationship studies of tubulysin analogs.
© Bentham Science Publishers