Zampanolide and Dactylolide: Cytotoxic Tubulin-Assembly Agents and Promising Anticancer Leads

TR Number

Date

2014-06-19

Journal Title

Journal ISSN

Volume Title

Publisher

The Royal Society of Chemistry

Abstract

Zampanolide is a marine natural macrolide and a recent addition to the family of microtubule-stabilizing cytotoxic agents. Zampanolide exhibits unique effects on tubulin assembly and is more potent than paclitaxel against several multi-drug resistant cancer cell lines. A high-resolution crystal structure of xB-tubulin in complex with zampanolide explains how taxane-site microtubule-stabilizing agents promote microtubule assemble and stability. This review provides an overview of current developments of zampanolide and its related but less potent analogue dactylolide, covering their natural sources and isolation, structure and conformation, cytotoxic potential, structure_activity studies, mechanism of action, and syntheses.

Description

Keywords

Zampanolide, Cytotoxic agents, Microtubule stabilizing agents, Multi-drug resistance, Anti-cancer drugs

Citation

Chen, Q.-H., & Kingston, D. G. I. (2014). Zampanolide and dactylolide: cytotoxic tubulin-assembly agents and promising anticancer leads. Natural Product Reports, 31(9), 1202-1226. doi: 10.1039/C4NP00024B