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.
- Standort
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Deutsche Nationalbibliothek Frankfurt am Main
- Umfang
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Online-Ressource
- Sprache
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Englisch
- Erschienen in
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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)
- Urheber
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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
- DOI
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10.1002/chem.202103520
- URN
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urn:nbn:de:101:1-2021113014040334888091
- Rechteinformation
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Letzte Aktualisierung
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15.08.2025, 07:33 MESZ
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Beteiligte
- 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
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