Maytansinol Functionalization: Towards Useful Probes for Studying Microtubule Dynamics
Zlata Boiarska
(1)
,
Helena Pérez‐peña
(2)
,
Anne‐catherine Abel
(3)
,
Paola Marzullo
(1)
,
Beatriz Álvarez‐bernad
(4)
,
Francesca Bonato
(1)
,
Benedetta Santini
(1)
,
Dragos Horvath
(5)
,
Daniel Lucena‐agell
(1)
,
Francesca Vasile
(1)
,
Maurizio Sironi
(1)
,
J. Fernando Díaz
(4)
,
Andrea E Prota
(3)
,
Stefano Pieraccini
(1)
,
Daniele Passarella
(1)
Dragos Horvath
- Fonction : Auteur
- PersonId : 178284
- IdHAL : dragos-horvath
- ORCID : 0000-0003-0173-5714
- IdRef : 108942368
Daniele Passarella
- Fonction : Auteur
- PersonId : 1295001
- ORCID : 0000-0001-6180-9581
Résumé
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.
Domaines
Chimie thérapeutiqueFormat du dépôt | Fichier |
---|---|
Type de dépôt | Article dans une revue |
Résumé |
en
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.
|
Titre |
en
Maytansinol Functionalization: Towards Useful Probes for Studying Microtubule Dynamics
|
Auteur(s) |
Zlata Boiarska
1
, Helena Pérez‐peña
2
, Anne‐catherine Abel
3
, Paola Marzullo
1
, Beatriz Álvarez‐bernad
4
, Francesca Bonato
1
, Benedetta Santini
1
, Dragos Horvath
5
, Daniel Lucena‐agell
1
, Francesca Vasile
1
, Maurizio Sironi
1
, J. Fernando Díaz
4
, Andrea E Prota
3
, Stefano Pieraccini
1
, Daniele Passarella
1
1
UNIMI -
Università degli Studi di Milano = University of Milan
( 300694 )
- Via Festa del Perdono 7 - 20122 Milano
- Italie
2
UNIMIB -
Università degli Studi di Milano-Bicocca = University of Milano-Bicocca
( 60273 )
- Piazza dell'Ateneo Nuovo, 1 - 20126, Milano
- Italie
3
PSI -
Paul Scherrer Institute
( 1961 )
- Villigen PSI, CH5232 Villigen, Suisse
- Suisse
4
CSIC -
Centro de Investigaciones Biológicas
( 41178 )
- Ramiro de Maeztu Madrid
- Espagne
5
CMC -
Chimie de la matière complexe
( 403339 )
- Institut Le Bel - 4, rue Blaise Pascal - 67070 STRASBOURG CEDEX
- France
|
Page/Identifiant |
e202203431
|
Langue du document |
Anglais
|
Nom de la revue |
|
Volume |
29
|
Numéro |
5
|
Vulgarisation |
Non
|
Comité de lecture |
Oui
|
Audience |
Internationale
|
Date de publication |
2022-12-05
|
Domaine(s) |
|
DOI | 10.1002/chem.202203431 |
Origine :
Fichiers produits par l'(les) auteur(s)
Loading...