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.
Keywords: Tubulysins, Anticancer agents, Total synthesis.
Mini-Reviews in Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/13895575113139990063 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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