Recent Advances in the Synthesis of Tubulysins

Title:Recent Advances in the Synthesis of Tubulysins

Volume: 13 Issue: 11

Author(s): Xu Xiangming, Gregory K. Friestad and Yao Lei

Affiliation:

Keywords: Tubulysins, Anticancer agents, Total synthesis.

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.

Cite this article as:

Xiangming Xu, Friestad K. Gregory and Lei Yao, Recent Advances in the Synthesis of Tubulysins, Mini-Reviews in Medicinal Chemistry 2013; 13 (11) . https://dx.doi.org/10.2174/13895575113139990063