Maytansinoids are a successful class of natural and semisynthetic tubulin binders, known for their potent cytotoxic activity. Their wider application as cytotoxins and chemical probes to study tubulin dynamics has been held back by the complexity of natural product chemistry. Here we report the synthesis of long-chain derivatives and maytansinoid conjugates. We confirmed that bulky substituents do not impact their high activity or the scaffold's binding mode. These encouraging results open new avenues for the design of new maytansine-based probes.

Boiarska, Z., Perez-Pena, H., Abel, A., Marzullo, P., Alvarez-Bernad, B., Bonato, F., et al. (2023). Maytansinol Functionalization: Towards Useful Probes for Studying Microtubule Dynamics. CHEMISTRY-A EUROPEAN JOURNAL, 29(5) [10.1002/chem.202203431].

Maytansinol Functionalization: Towards Useful Probes for Studying Microtubule Dynamics

Santini B.;
2023

Abstract

Maytansinoids are a successful class of natural and semisynthetic tubulin binders, known for their potent cytotoxic activity. Their wider application as cytotoxins and chemical probes to study tubulin dynamics has been held back by the complexity of natural product chemistry. Here we report the synthesis of long-chain derivatives and maytansinoid conjugates. We confirmed that bulky substituents do not impact their high activity or the scaffold's binding mode. These encouraging results open new avenues for the design of new maytansine-based probes.
Articolo in rivista - Articolo scientifico
chemical probes; maytansinoids; maytansinol functionalization; microtubules; tubulin;
English
5-dic-2022
2023
29
5
e202203431
partially_open
Boiarska, Z., Perez-Pena, H., Abel, A., Marzullo, P., Alvarez-Bernad, B., Bonato, F., et al. (2023). Maytansinol Functionalization: Towards Useful Probes for Studying Microtubule Dynamics. CHEMISTRY-A EUROPEAN JOURNAL, 29(5) [10.1002/chem.202203431].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/497299
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