Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders

Abstract: Maytansinol is a valuable precursor for the preparation of maytansine derivatives (known as maytansinoids). Inspired by the intriguing structure of the macrocycle and the success in targeted cancer therapy of the derivatives, we explored the maytansinol acylation reaction. As a result, we were able to obtain a series of derivatives with novel modifications of the maytansine scaffold. We characterized these molecules by docking studies, by a comprehensive biochemical evaluation, and by determination of their crystal structures in complex with tubulin. The results shed further light on the intriguing chemical behavior of maytansinoids and confirm the relevance of this peculiar scaffold in the scenario of tubulin binders.

Object Details

• Location: Deutsche Nationalbibliothek Frankfurt am Main
• Extent: Online-Ressource
• Language: Englisch

References and Relationships

• Bibliographic citation: Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders ; day:29 ; month:11 ; year:2021 ; extent:1 ; Chemistry - a European journal ; (29.11.2021) (gesamt 1)

Contributors, Places and Time

• Creator: Marzullo, Paola ; Boiarska, Zlata ; Pérez‐Peña, Helena ; Abel, Anne‐Catherine ; Álvarez‐Bernad, Beatriz ; Lucena‐Agell, Daniel ; Vasile, Francesca ; Sironi, Maurizio ; Altmann, Karl‐Heinz ; Prota, Andrea E. ; Díaz, J. Fernando ; Pieraccini, Stefano ; Passarella, Daniele

Further information

• DOI: 10.1002/chem.202103520
• URN: urn:nbn:de:101:1-2021113014040334888091
• Rights: Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
• Last update: 15.08.2025, 7:33 AM CEST